The immune system has evolved to survey and respond appropriately to the universe of foreign pathogens, deploying an intricate repertoire of mechanisms that keep responses to host tissues in check. The immune system is typically divided into two categories--innate and adaptive. Innate immunity refers to nonspecific defense mechanisms that come into play immediately or within hours of an antigen's appearance in the body. Adaptive immunity refers to antigen-specific immune response. The antigen first must be processed and recognized, and then the adaptive immune system creates an army of immune cells specifically designed to attack that antigen. For the adaptive immune system, specificity and sensitivity are provided by a large repertoire of antigen T-cell receptors (TCRs) constructed in their extracellular domain to recognize antigenic peptide fragments restricted and presented by histocompatibility complex molecules, and coupled through intracellular domains to signal transduction modules that serve to transmit environmental cues inside the cell.

Inflammation is triggered when innate immune cells detect infection or tissue injury. Pattern recognition receptors (PRRs) respond to pathogen-associated molecular patterns (PAMPs) or host-derived damage-associated molecular patterns (DAMPs) by triggering activation of NF-κB, AP1, CREB, c/EBP, and IRF transcription factors. Induction of genes encoding enzymes, chemokines, cytokines, adhesion molecules, and regulators of the extracellular matrix promotes the recruitment and activation of leukocytes. Besides resolving infection and injury, chronic inflammation is a risk factor for cancer.

Immunity has a major impact on inflammatory diseases and cancer, and biologics targeting immune cells and their factors. Immunosuppressant drugs suppress, or reduce, the strength of the body’s immune system, and have been used in the treatment of organ transplantation or autoimmunine diseases. Immunomodulator drugs have contributed to the significant improvement against cancer and other related diseases.

References:
[1] Sakaguchi S, et al. Immunol Cell Biol. 2012 Mar;90(3):277-87. doi: 10.1038/icb.2012.4.
[2] Newton K, et al. Cold Spring Harb Perspect Biol. 2012 Mar; 4(3): a006049.
[3] Bartneck M. Macromol Biosci. 2017 Apr 6. doi: 10.1002/mabi.201700021.


Anti-infection >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
Autophagy LRRK2 ULK Mitophagy
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Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
Cytoskeleton >
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Epigenetics >
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GPCR/G Protein >
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Immunology/Inflammation >
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JAK/STAT Signaling >
EGFR JAK Pim STAT
MAPK/ERK Pathway >
ERK JNK KLF MAP3K MAP4K MAPKAPK2 (MK2) MEK Mixed Lineage Kinase MNK p38 MAPK Raf Ribosomal S6 Kinase (RSK)
Membrane Transporter/Ion Channel >
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Metabolic Enzyme/Protease >
15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
Neuronal Signaling >
5-HT Receptor AChE Adenosine Kinase Amyloid-β Beta-secretase CaMK CGRP Receptor COMT Dopamine Receptor Dopamine Transporter FAAH GABA Receptor GlyT iGluR Imidazoline Receptor mAChR Melatonin Receptor Monoamine Oxidase nAChR Neurokinin Receptor Opioid Receptor Serotonin Transporter γ-secretase
NF-κB >
NF-κB IKK Keap1-Nrf2 MALT1
PI3K/Akt/mTOR >
Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
PROTAC E3 Ligase Ligand-Linker Conjugate Ligand for E3 Ligase PROTAC Linker PROTAC-linker Conjugate for PAC
Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
Stem Cell/Wnt >
Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
TGF-beta/Smad >
TGF-beta/Smad PKC ROCK TGF-β Receptor
Vitamin D Related >
VD/VDR
Others >
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PS372424 hydrochloride

PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation[1][2].

  • CAS Number: 1596362-29-6
  • MF: C33H45ClN6O4
  • MW: 625.20
  • Catalog: CXCR
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sulindac

Sulindac is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.

  • CAS Number: 38194-50-2
  • MF: C20H17FO3S
  • MW: 356.411
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 581.6±50.0 °C at 760 mmHg
  • Melting Point: 182-185°C
  • Flash Point: 305.6±30.1 °C

Ulevostinag (isomer 1)

Ulevostinag isomer 1 (MK-1454 isomer 1) is the isomer of Ulevostinag. Ulevostinag is a STING agonist[1].

  • CAS Number: 2231258-61-8
  • MF: C20H22F2N10O9P2S2
  • MW: 710.52
  • Catalog: STING
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ibuprofen Impurity F

Ibuprofen Impurity F is an Ibuprofen impurity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively[1].

  • CAS Number: 65322-85-2
  • MF: C13H18O2
  • MW: 206.28100
  • Catalog: COX
  • Density: 1.034 g/cm3
  • Boiling Point: 327.445ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 224.48ºC

GDC-2394

GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation[1][2].

  • CAS Number: 2238822-07-4
  • MF: C20H25N5O4S
  • MW: 431.51
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Faralimomab

Faralimomab (64G12) is an immunomodulator, and a murine anti-IFNA1 IgG1 mAb[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Phenyl β-D-glucopyranoside

Phenyl β-D-glucopyranoside has anti-cancer and anti-inflammatory activities. Phenyl β-D-glucopyranoside inhibits nitric oxide (NO) production, and the expression of iNOS and COX-2. Phenyl β-D-glucopyranoside also inhibits the nuclear translocation of NF-κB[1].

  • CAS Number: 1464-44-4
  • MF: C12H16O6
  • MW: 256.25
  • Catalog: COX
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 482.1±45.0 °C at 760 mmHg
  • Melting Point: 176-178ºC(lit.)
  • Flash Point: 245.4±28.7 °C

Isothipendyl

Isothipendyl (AY 56012), an azaphenothiazine derivative, is a potent histamine 1 (H1) receptor antagonist. Isothipendyl is a primary metabolite[1].

  • CAS Number: 482-15-5
  • MF: C16H19N3S
  • MW: 285.40700
  • Catalog: Histamine Receptor
  • Density: 1.167g/cm3
  • Boiling Point: 421.3ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 208.6ºC

Monalizumab

Monalizumab is a first-in-class immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC)[1][2].

  • CAS Number: 1228763-95-8
  • MF:
  • MW:
  • Catalog: Checkpoint Kinase (Chk)
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pitolisant

Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).

  • CAS Number: 362665-56-3
  • MF: C17H26ClNO
  • MW: 295.84700
  • Catalog: Histamine Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RO2959 monohydrochloride

RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways[1][2].

  • CAS Number: 2309172-44-7
  • MF: C21H20ClF2N5OS
  • MW: 463.93
  • Catalog: Interleukin Related
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Levilimab

Levilimab (BCD-089) is a fully human anti-interleukin-6 receptor (IL-6R) monoclonal antibody. Levilimab is an inflammation-alleviating antibody. Levilimab can be used for the research of rheumatoid[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

bromazine

Bromodiphenhydramine (Ambodryl) is a potent antihistamine with antimicrobial property. Bromodiphenhydramine inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine can be used for cutaneous allergies research[1][2][3].

  • CAS Number: 118-23-0
  • MF: C17H20BrNO
  • MW: 334.25100
  • Catalog: Bacterial
  • Density: 1.259g/cm3
  • Boiling Point: 397.3ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 194.1ºC

Nyasol

Nyasol ((-)-Nyasol) is an active compound that has antifungal, antibacterial, antileishmanial, hyaluronidase inhibition activities. Nyasol inhibits LTB4 binding to human neutrophils. Nyasol suppresses neuroinflammatory response through the inhibition of I-κB degradation in LPS (HY-D1056)-stimulated BV-2 microglial cells[1][2].

  • CAS Number: 96895-25-9
  • MF: C17H16O2
  • MW: 252.31
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Aminopicoline

Aminopicoline (Ascensil) is a potent and nonselective inhibitor of NO synthase (NOS) isoenzymes (iNOS, nNOS, eNOS)[1].

  • CAS Number: 695-34-1
  • MF: C6H8N2
  • MW: 108.141
  • Catalog: NO Synthase
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 227.4±20.0 °C at 760 mmHg
  • Melting Point: 96-99 °C(lit.)
  • Flash Point: 114.0±9.0 °C

Decloxizine (dihydrochloride)

Decloxizine dihydrochloride(UCB-1402; NSC289116) is a histamine 1 receptor antagonist.

  • CAS Number: 13073-96-6
  • MF: C21H30Cl2N2O2
  • MW: 413.38100
  • Catalog: Histamine Receptor
  • Density: 1.115g/cm3
  • Boiling Point: 472.4ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 239.5ºC

PROTAC IRAK4 degrader-3

PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader[1].

  • CAS Number: 2374122-43-5
  • MF: C57H68FN11O8S
  • MW: 1086.28
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BECLOMETASONE DIPROPIONATE MONOHYDRATE

Beclometasone dipropionate monohydrate, the prodrug of Beclometasone, is an orally active and potent glucocorticoid recepter agonist. Beclometasone dipropionate monohydrate acts via a glucocorticoid receptor and suppresses inflammation and hyperproliferation. Beclometasone dipropionate monohydrate can be used for asthma [1][2].

  • CAS Number: 77011-63-3
  • MF: C34H51ClO12
  • MW: 687.21500
  • Catalog: Glucocorticoid Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Broussonin E

Broussonin E is a phenolic compound and shows anti-inflammatory activity. Broussonin E can suppress inflammation by modulating macrophages activation statevia inhibiting the ERK and p38 MAPK and enhancing JAK2-STAT3 signaling pathway. Broussonin E can be used for the research of inflammation-related diseases such as atherosclerosis[1].

  • CAS Number: 90902-21-9
  • MF: C17H20O4
  • MW: 288.338
  • Catalog: JAK
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 464.9±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 235.0±27.3 °C

Decloxizine

Decloxizine(UCB-1402; NSC289116) is a histamine 1 receptor antagonist.

  • CAS Number: 3733-63-9
  • MF: C21H28N2O2
  • MW: 340.459
  • Catalog: Histamine Receptor
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 472.4±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 239.5±27.3 °C

Anemonine

Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases[1][2].

  • CAS Number: 508-44-1
  • MF: C10H8O4
  • MW: 192.17
  • Catalog: PKC
  • Density: 1.45
  • Boiling Point: 535.7ºC at 760 mmHg
  • Melting Point: 157-158ºC
  • Flash Point: 300.7ºC

Peresolimab

Peresolimab is a humanized IgG1-κ antibody targeting to PD-1. Peresolimab potentially stimulates physiological immune inhibitory pathways to restore immune homeostasis[1][2].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propanedioic acid,2-[(2-nitrophenyl)methylene]-, 1,3-dimethyl ester

NCI126224 is a TLR4 signaling inhibitor. NCI126224 suppress LPS (HY-D1056)-induced production of NF-κB, TNF-α, IL-1β, and NO in the nanomolar-low micromolar range. NCI126224 can be used for the research of inflammatory diseases[1].

  • CAS Number: 65974-52-9
  • MF: C12H11NO6
  • MW: 265.21900
  • Catalog: Toll-like Receptor (TLR)
  • Density: 1.335g/cm3
  • Boiling Point: 361.7ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 151.8ºC

ALR-27

ALR-27 is an antagonist of the 5-lipoxygenase (5-LOX) activating protein FLAP and has anti-inflammatory activity. ALR-27 potently inhibits 5-LOX product formation (>80%) in pro-inflammatory M1-MDM, with no significant direct inhibition of 5-LOX. ALR-27 not only reduces prostaglandin and leukotriene (LT) production in neutrophils but also increases the production of specialized prolytic mediators in specific human macrophage phenotypes[1].

  • CAS Number: 903639-13-4
  • MF: C19H22O3
  • MW: 298.38
  • Catalog: FLAP
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BCX 1470 (methanesulfonate)

BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.IC50 Value: 96 nM (Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1]Target: Factor D; C1sBCX 1470(Thrombin inhibitor) is serine protease inhibitor.BCX 1470(Thrombin inhibitor) blocks the esterolytic and hemolytic activities of the complement enzymes Cls and factor D in vitro, also blocked development of RPA-induced edema in the rat.

  • CAS Number: 217099-44-0
  • MF: C15H14N2O5S3
  • MW: 398.47700
  • Catalog: Complement System
  • Density: N/A
  • Boiling Point: 509.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 262.2ºC

Risankizumab

Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis[1][2][3].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

STING agonist-23

STING agonist-23 (CF502) is a non-nucleotide small-molecule STING agonist. STING agonist-23 activates STING, increases phosphorylation of STING, TBK1 and IRF3. STING agonist-23 promotes the levels of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. STING agonist-23 exhibits activity against SARS-CoV series strains[1].

  • CAS Number: 2361570-16-1
  • MF: C33H35N13O4
  • MW: 677.72
  • Catalog: STING
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acetaminophen-13C2,15N

Acetaminophen-13C2,15N is the 13C and 15N labeled Acetaminophen[1]. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent[2][3][4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[5].

  • CAS Number: 360769-21-7
  • MF: C613C2H915NO2
  • MW: 154.14
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Diclofenac Epolamine

Flector Patch (Diclofenac epolamine) is a non-steroidal anti-inflammatory drug (NSAID)[1]. Flector Patch is used for relieving arthritis Pain, acute Pain, osteoarthritis, and actinic Keratosis. Flector Patch has good skin absorption characteristics without local adverse reactions and allergies[2].

  • CAS Number: 119623-66-4
  • MF: C20H24Cl2N2O3
  • MW: 411.32
  • Catalog: COX
  • Density: N/A
  • Boiling Point: 412ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 203ºC

Benvitimod (Tapinarof)

Tapinarof is a natural aryl hydrocarbon receptor (AhR) agonist with an EC50 of 13 nM.

  • CAS Number: 79338-84-4
  • MF: C17H18O2
  • MW: 254.32400
  • Catalog: Aryl Hydrocarbon Receptor
  • Density: 1.158
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A