Thrombin is a serine protease that in humans is encoded by the F2 gene. Thrombin is an intriguing coagulation protease demonstrating an array of effects on endothelial cells, vascular smooth muscle cells (VSMC), monocytes, and platelets, all of which are involved in the pathophysiology of atherosclerosis. There is mounting evidence that thrombin acts as a powerful modulator of many processes like regulation of vascular tone, permeability, migration and proliferation of VSMC, recruitment of monocytes into the atherosclerotic lesions, induction of diverse pro-inflammatory markers, and all of these are related to the progression of cardiovascular disease. Recent studies in transgenic mice models indicate that the deletion of the natural thrombin inhibitor heparin cofactor II promotes an accelerated atherogenic state. The combined evidence points to thrombin as a pivotal contributor to vascular pathophysiology. Considering the clinical development of selective anticoagulants including direct thrombin inhibitors.


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Dabigatran etexilate mesylate

Dabigatran etexilate mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]in vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1

  • CAS Number: 872728-81-9
  • MF: C35H45N7O8S
  • MW: 723.839
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dabigatran etexilate

Dabigatran etexilate(BIBR-1048) is the orally active prodrug of dabigatran; Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]in vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1

  • CAS Number: 211915-06-9
  • MF: C34H41N7O5
  • MW: 627.733
  • Catalog: Thrombin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 827.9±75.0 °C at 760 mmHg
  • Melting Point: 128-129°
  • Flash Point: 454.5±37.1 °C

Sofigatran

Sofigatran (MCC-977) is an orally active factor IIa (thrombin) inhibitor, acts as an anticoagulant. Sofigatran is used for the research of cardiovascular disease[1].

  • CAS Number: 187602-11-5
  • MF: C24H44N4O4S
  • MW: 484.69600
  • Catalog: Thrombin
  • Density: 1.118
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NP-313

NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca2+ inward flow[1].

  • CAS Number: 5397-78-4
  • MF: C12H8ClNO3
  • MW: 249.65000
  • Catalog: Thrombin
  • Density: 1.44g/cm3
  • Boiling Point: 427.7ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 212.5ºC

Metolazone

Metolazone(Zaroxolyn) is primarily used to treat congestive heart failure and high blood pressure.Target: OthersMetolazone is a thiazide-like diuretic marketed under the brand names Zytanix from Zydus Cadila, Zaroxolyn, and Mykrox. It is primarily used to treat congestive heart failure and high blood pressure. Metolazone indirectly decreases the amount of water reabsorbed into the bloodstream by the kidney, so that blood volume decreases and urine volume increases. This lowers blood pressure and prevents excess fluid accumulation in heart failure. Metolazone is sometimes used together with loop diuretics such as furosemide or bumetanide, but these highly effective combinations can lead to dehydration and electrolyte abnormalities.Metolazone and the other thiazide diuretics inhibit the function of the sodium-chloride symporter, preventing sodium and chloride, and therefore water too, from leaving the lumen to enter the tubule cell. As a result, water remains in the lumen and is excreted as urine, instead of being reabsorbed into the bloodstream. Since most of the sodium in the lumen has already been reabsorbed by the time the filtrate reaches the distal convoluted tubule, thiazide diuretics have limited effects on water balance and on electrolyte levels. Nevertheless, they can be associated with low sodium levels, volume depletion, and low blood pressure, among other adverse effects.

  • CAS Number: 17560-51-9
  • MF: C16H16ClN3O3S
  • MW: 365.835
  • Catalog: Thrombin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 613.6±65.0 °C at 760 mmHg
  • Melting Point: 252-254°C
  • Flash Point: 324.9±34.3 °C

Atecegatran metoxil

Atecegatran metoxil is a oral anticoagulant, which inhibits thrombin factor II and is used in thromboembolic disorders. In vivo, Atecegatran metoxil is converted to AR-H067637, a selective and reversible direct thrombin inhibitor.

  • CAS Number: 433937-93-0
  • MF: C22H23ClF2N4O5
  • MW: 496.89200
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Melagatran

Melagatran is a direct and oral active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin. Melagatran does not require endogenous co-factors for its antithrombin effect and may help to alleviate some of the damaging effects of endotoxemia[1]. Melagatran has the potential to provide a rational approach in the prevention of arterial occlusion[2].

  • CAS Number: 159776-70-2
  • MF: C22H31N5O4
  • MW: 429.51300
  • Catalog: Thrombin
  • Density: 1.41g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(10β)-10,18-Epoxyros-15-ene-7,18-dione

Rosenonolactone shows inhibitory activity against prolyl endopeptidase and thrombin and cholesterol ester transfer protein[1][2][3].

  • CAS Number: 508-71-4
  • MF: C20H28O3
  • MW: 316.43
  • Catalog: CETP
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 449.0±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 196.2±28.8 °C

Thrombin inhibitor 1

Thrombin inhibitor 1 is a potent thrombin inhibitor (Ki=0.66 nM, 2xaPTT=0.43 μM).

  • CAS Number: 855998-46-8
  • MF: C22H20Cl2F2N4O3
  • MW: 497.32
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thrombin receptor peptide ligand

Thrombin receptor peptide ligand is a thrombin receptor antagonist peptide that can be used as an antithrombotic agent[1].

  • CAS Number: 287964-20-9
  • MF: C33H54N10O8
  • MW: 718.84
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Argatroban

Argatroban monohydrate is a direct, selective thrombin inhibitor.Target: ThrombinArgatroban may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Administration (0.5 to 2 micrograms/kg/min) of argatroban is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries [1]. Argatroban, as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation. The incidences of major bleeding and adverse clinical outcome were lower in the patients receiving argatroban [2].

  • CAS Number: 141396-28-3
  • MF: C23H38N6O6S
  • MW: 526.65
  • Catalog: Thrombin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 801.3±75.0 °C at 760 mmHg
  • Melting Point: -41.5 °C
  • Flash Point: 438.4±37.1 °C

N-[(1S,2R,4S)-4-carbamoyl-2-[(7-methyl-4,5,6,8-tetrahydropyrido[4,3-e][1,3]thiazine-2-carbonyl)amino]cyclohexyl]-N'-(5-chloropyridin-2-yl)oxamide,hydrochloride

Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research[1].

  • CAS Number: 480448-29-1
  • MF: C23H29Cl2N7O4S
  • MW: 570.49200
  • Catalog: Factor Xa
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aeruginosin 98-B

Aeruginosin 98-B is a protease inhibitor. Aeruginosin 98-B inhibits trypsin, plasmin and thrombin with IC50 values of 0.6, 7.0 and 10.0 μg/mL, respectively[1].

  • CAS Number: 167228-01-5
  • MF: C29H46N6O9S
  • MW: 654.77500
  • Catalog: Protease-Activated Receptor (PAR)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bivalirudin trifluoroacetate salt

Bivalirudin Trifluoroacetate is a synthetic 20 residue peptide which reversibly inhibits thrombin.IC50 Value:Target: thrombinin vitro: Eptifibatide (8 mg/mL) added together with a low (70 ng/mL) concentration of bivalirudin (a direct thrombin inhibitor) effectively (approximately 90%) reduced platelet aggregation induced by thrombin (0.2 U/mL) [1]. In thrombin generation assay (TGA), bivalirudin had no effect on these parameters up to 10 μmol/l [2]. Bivalirudin-facilitated binding of MPO to BAEC resulted also in functional changes in terms of increased NO consumption as well as enhanced MPO-mediated redox modifications [3].in vivo: The use of bivalirudinprevented further increase in antiheparin/PF4 antibody IgG levels in rats [4]. Three animals in the 500-mg/kg/24 h group, and 7 animals in the 2000-mg/kg/24 h group in the toxicokinetic assessment phase of the study were found dead or euthanized in extremis (following blood sampling). Plasma concentrations of bivalirudin appeared to be linear and dose independent [5].Clinical trial: Antithrombotic Effects of Ticagrelor Versus Clopidogrel . Phase 4

  • CAS Number: 128270-60-0
  • MF: C98H138N24O33
  • MW: 2295.31
  • Catalog: Peptides
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Napsagatran hydrate

Napsagatran hydrate is a novel and specific thrombin inhibitor.

  • CAS Number: 159668-20-9
  • MF: C26H36N6O7S
  • MW: 576.66500
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dabigatran (BIBR 953)

Dabigatran(BIB-953; BIBR 953ZW) is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]Target: thrombinin vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1

  • CAS Number: 211914-51-1
  • MF: C25H25N7O3
  • MW: 471.511
  • Catalog: Thrombin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 797.1±70.0 °C at 760 mmHg
  • Melting Point: 268-272ºC
  • Flash Point: 435.9±35.7 °C

Dabigatran (ethyl ester hydrochloride)

Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and a thrombin inhibitor.

  • CAS Number: 211914-50-0
  • MF: C27H30ClN7O3
  • MW: 536.025
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Idraparinux sodium

Idraparinux (sodium) is a polymethylated synthetic pentasaccharide known to interact with the antithrombin III and act as anticoagulant.

  • CAS Number: 149920-56-9
  • MF: C38H55Na9O49S7
  • MW: 1727.177
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sar-Pro-Arg-pNA hydrochloride salt

Sar-Pro-Arg-pNA is a chromogenic substrate of α-thrombin. Sar-Pro-Arg-pNA can be used to test α-thrombin activity[1].

  • CAS Number: 77695-30-8
  • MF: C20H30N8O5
  • MW: 462.50
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HIRUDIN LEECH, RECOMBINANT

Hirudin is a Thrombin inhibitor with blood anticoagulant property. Hirudin has potent anti-thrombotic, wound repair, anti-fibrosis, anti-tumor and anti-hyperuricemia effects. Hirudin also affects diabetic complications, cerebral hemorrhage, and others[1].

  • CAS Number: 8001-27-2
  • MF: C287H440N80O110S6
  • MW: 7027
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Razaxaban hydrochloride

Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity[1].

  • CAS Number: 405940-76-3
  • MF: C24H21ClF4N8O2
  • MW: 564.92300
  • Catalog: Factor Xa
  • Density: N/A
  • Boiling Point: 654.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 349.8ºC

Lepirudin acetate salt

Lepirudin is a potent irreversible thrombin inhibitor. Lepirudin also is a recombinant hirudin. Lepirudin has anticoagulation in heparin-induced thrombocytopenia (HIT)[1].

  • CAS Number: 138068-37-8
  • MF: C287H446N80O111S6
  • MW: 6979.486
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 65 °C
  • Flash Point: N/A

Edoxaban-d6

Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment[1][2][3].

  • CAS Number: 1304701-57-2
  • MF: C24H24D6ClN7O4S
  • MW: 554.09
  • Catalog: Factor Xa
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-Gly-Pro-Arg-4MβNA acetate salt

Z-Gly-Pro-Arg-4MβNA is the cleavage of the substrate of thrombin to release free 4-methoxy-2-naphthylamine (4MβNA). Free 4MβNA can be captured by 5-nitrosalicylaldehyde to produce an insoluble yellow fluorescent and marks the site of thrombin activity[1].

  • CAS Number: 66647-41-4
  • MF: C32H39N7O6
  • MW: 617.70
  • Catalog: Thrombin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Enoxaparin sodium

Enoxaparin (PK 10169), a low-molecular-weight heparin (LMWH) derivative. Enoxaparin exerts anticoagulant activity through antithrombin III, an endogenous inhibitor of factor Xa and thrombin IIa. Enoxaparin protect the rat hippocampus against TBI (traumatic brain injury) via antioxidant and anti-inflammatory properties. Enoxaparin can be used for the research of deep vein thrombosis (DVT), pulmonary embolism, TBI and COVID-19[1][2][3].

  • CAS Number: 679809-58-6
  • MF: C26H42N2O37S5
  • MW: 1134.92788
  • Catalog: SARS-CoV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAY 1217224

BAY 1217224 is a neutral, non-prodrug Thrombin inhibitor with good oral pharmacokinetics.

  • CAS Number: 1639886-32-0
  • MF: C24H27ClFN3O5
  • MW: 491.94
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dabigatran (ethyl ester)

ethyl ester of Dabigatran, which is an emerging oral anticoagulant which is a direct inhibitor of thrombin activity. IC50 value:Target: thrombinDabigatran provides a stable anticoagulation effect without any need to perform periodical laboratory controls. Of note, there is a growing amount of clinical evidence which shows its safety and efficacy. For these reasons, Dabigatran may suppose a revolution in oral anticoagulation. Dabigatran etexilate was rapidly converted to Dabigatran, with peak plasma dabigatran concentrations being attained after approximately 1.5 h; the bioavailability of Dabigatran after p.o. administration of Dabigatran etexilate was 7.2%.

  • CAS Number: 429658-95-7
  • MF: C27H29N7O3
  • MW: 499.564
  • Catalog: Thrombin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 759.5±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 413.1±35.7 °C

15,16-Dihydrotanshindiol C

15,16-Dihydrotanshindiol C, a diterpenoid, is a potent thrombin inhibitor[1][2].

  • CAS Number: 891854-96-9
  • MF: C18H18O5
  • MW: 314.332
  • Catalog: Thrombin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 534.6±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 198.3±23.6 °C

Desirudin

Desirudin (CGP 39393) is a thrombin inhibitor. Desirudin can inhibit the formation of blood clots and venous stasis thrombosis, which is used for the research of thrombocytopenia or platelet dysfunction[1][2].

  • CAS Number: 120993-53-5
  • MF: C287H440N80O110S6
  • MW:
  • Catalog: Thrombin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Protamine sulfates

Protamine sulfate, polycationic peptide and a antiheparin agent, could neutralize the anticoagulant action of heparin and enhances lipid-mediated gene transfer[1][2][3].

  • CAS Number: 9009-65-8
  • MF: C264H460N128O65S7
  • MW: 6691.85629
  • Catalog: Thrombin
  • Density: 2.2±0.1 g/cm3
  • Boiling Point: 330.0±11.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: N/A