Carbonic anhydrase is a zinc-containing enzyme that catalyzes the reversible hydration of carbon dioxide: CO2+H2O<-->HCO3-+H+. The enzyme is the target for drugs, such as Acetazolamide, Methazolamide, and Dichlorphenamide, for the treatment of glaucoma. There are three evolutionarily unrelated CA families, designated alpha, beta, and gamma. All known CAs from the animal kingdom are of the alpha type. There are seven mammalian CA isozymes with different tissue distributions and intracellular locations, CA I-VII. Carbonic anhydrase is one of the core enzyme in organism, which involves in osmoregulation, ionic regulation, acid-base regulation and other physiological and biochemical process.


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Sultiame

Sultiame is a carbonic anhydrase inhibitor, widely used as an antiepileptic drug.

  • CAS Number: 61-56-3
  • MF: C10H14N2O4S2
  • MW: 290.35900
  • Catalog: Carbonic Anhydrase
  • Density: 1.472g/cm3
  • Boiling Point: 520.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 268.4ºC

indisulam

Indisulam (E 7070) is a carbonic anhydrase inhibitor and a G1-targeting agent. Indisulam causes a blockade in the G1/S transition through inhibition of the activation of both cyclin-dependent kinase 2 (CDK2) and cyclin E. Shows anti-tumor activity in human colon and lung cancer cells[1][2].

  • CAS Number: 165668-41-7
  • MF: C14H12ClN3O4S2
  • MW: 385.846
  • Catalog: Carbonic Anhydrase
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 668.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 358.4±34.3 °C

Acetazolamide D3

Acetazolamide D3 is deuterium labeled Acetazolamide, which is a potent carbonic anhydrase (CA) inhibitor.

  • CAS Number: 1189904-01-5
  • MF: C4H3D3N4O3S2
  • MW: 225.26400
  • Catalog: Carbonic Anhydrase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methazolamide

Methazolamide is a carbonic anhydrase inhibitor used to treat glaucoma.Target: Carbonic AnhydraseMethazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively [1]. Methazolamide is of strength equal to acetazolamide, another carbonic anhydrase inhibitor used to treat irregular breathing disorders. However, methazolamide differs from acetazolamide in that it fails to activate Ca2+-dependent potassium channels in skeletal muscles. Methazolamide does not impair respiratory work performance in anesthetized rabbits [2]. Oral administration of methazolamide decreases IOPs and AHFRs in clinically normal dogs, with effectiveness diminishing in the evening [3].

  • CAS Number: 554-57-4
  • MF: C5H8N4O3S2
  • MW: 236.272
  • Catalog: Carbonic Anhydrase
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: 402.0±28.0 °C at 760 mmHg
  • Melting Point: 208ºC (dec.)
  • Flash Point: 196.9±24.0 °C

2-Aminobenzenesulfonamide

2-Aminobenzenesulfonamide is a carbonic anhydrase IX inhibitor.

  • CAS Number: 3306-62-5
  • MF: C6H8N2O2S
  • MW: 172.205
  • Catalog: Carbonic Anhydrase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 392.7±44.0 °C at 760 mmHg
  • Melting Point: 155-157 °C(lit.)
  • Flash Point: 191.3±28.4 °C

U-104

U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.IC50 value: 45.1 nM/4.5 nM(Ki, CA IX/CA XII) [1]Target: Carbonic anhydrase inhibitorin vitro: U-104 (50 μM) blocks the mesenchymal phenotype in the cancer stem cells population in hypoxia condition of 4T1 cells. U-104 (<50 μM) significantly reduces migration in a dose-dependent manner in metastatic MDA-MB-231 LM2-4Luc+ cells , with cells growing as compact colonies similar to parental MDA-MB-231 cells [2]. in vivo: U-104 (38 mg/kg) inhibits primary tumor growth in the mice implanted orthotopically with MDA-MB-231 LM2-4Luc+ cells. U-104 (19 mg/kg) inhibits metastases formation in the 4T1 experimental metastasis mice model [1]. U-104 (38 mg/kg) significantly delay primary tumor growth and reduces cancer stem cell population in NOD/SCID mice orthotopically implanted with MDA-MB-231 LM2-4Luc+ cells. U-104 (5 mg/mL, oral gavage) shows a significant delay in tumor growth in Balb/c mice orthotopically implanted with 4T1 cells [2].

  • CAS Number: 178606-66-1
  • MF: C13H12FN3O3S
  • MW: 309.316
  • Catalog: Carbonic Anhydrase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 242-243℃
  • Flash Point: N/A

Benzthiazide

Benzthiazide is a long-acting diuretic[1] and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells[2].

  • CAS Number: 91-33-8
  • MF: C15H14ClN3O4S3
  • MW: 431.93700
  • Catalog: Carbonic Anhydrase
  • Density: 1.4176 (rough estimate)
  • Boiling Point: N/A
  • Melting Point: 231-232° (U.S. patent); mp 238-239° (P'an)
  • Flash Point: N/A

acetazolamide

Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX[1]. Diuretic effects[4].

  • CAS Number: 59-66-5
  • MF: C4H6N4O3S2
  • MW: 222.245
  • Catalog: Autophagy
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 256-261°C
  • Flash Point: N/A

Ethoxzolamide

Ethoxzolamide is a carbonic anhydrase inhibitor with Ki of 1 nM.

  • CAS Number: 452-35-7
  • MF: C9H10N2O3S2
  • MW: 258.31700
  • Catalog: Carbonic Anhydrase
  • Density: 1.47g/cm3
  • Boiling Point: 464.9ºC at 760mmHg
  • Melting Point: 190-193ºC(lit.)
  • Flash Point: 235ºC

diclofenamide

Dichlorphenamide(Diclofenamide) is a carbonic anhydrase inhibitor that is used in the treatment of glaucoma. Target: Carbonic AnhydraseDichlorphenamide is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class. This drug has the same side-effects as acetazolamide, for which it is a useful substitute, except for a lesser tendency to cause dermatitis, renal calculi and metabolic acidosis. It may induce a more pronounced renal loss of potassium [1]. An average daily dose of 33 mg of diclofenamide, a carbonic-anhydrase inhibitor, was added to the anti-epileptic medication already employed in 105 cases of severe epilepsy which had shown insufficient clinical improvement. A favourable action on seizures, often accompanied by an improvement in the EEG tracing, was observed in 83 cases. The effect was of long duration in 47 cases in that it lasted for more than a year. It persisted for one to twelve months in a further 17 cases, while in 19 patients, who had reacted favourably to the treatment, medication had to be suspended because of intolerance [2].

  • CAS Number: 120-97-8
  • MF: C6H6Cl2N2O4S2
  • MW: 305.159
  • Catalog: Carbonic Anhydrase
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: 590.5±60.0 °C at 760 mmHg
  • Melting Point: 239-241ºC
  • Flash Point: 310.9±32.9 °C

tioxolone

Tioxolone, a metalloenzyme carbonic anhydrase I inhibitor, is an anti-acne preparation.Target: Carbonic Anhydrase Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor with a Ki of 91 nM. Tioxolone lacks sulfonamide, sulfamate, or hydroxamate functional groups that are typically found in therapeutic carbonic anhydrase (CA) inhibitors, such as acetazolamide. Tioxolone is proposed to be a prodrug inhibitor that is cleaved via a CA II zinc-hydroxide mechanism known to catalyze the hydrolysis of esters. When tioxolone binds in the active site of CA II, it is cleaved and forms 4-mercaptobenzene-1,3-diol via the intermediate S-(2,4-thiophenyl) hydrogen thiocarbonate. The esterase cleavage product binds to the zinc active site via the thiol group and is therefore the active CA inhibitor, while the intermediate is located at the rim of the active-site cavity. From Wikipedia.

  • CAS Number: 4991-65-5
  • MF: C7H4O3S
  • MW: 168.170
  • Catalog: Carbonic Anhydrase
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 377.8±44.0 °C at 760 mmHg
  • Melting Point: 158-160 °C(lit.)
  • Flash Point: 182.3±28.4 °C

Brinzolamide

Brinzolamide(AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.Target: carbonic anhydrase IIBrinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1-2 hours. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice [1]. Brinzolamide (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily [2].

  • CAS Number: 138890-62-7
  • MF: C12H21N3O5S3
  • MW: 383.507
  • Catalog: Carbonic Anhydrase
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 586.0±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 308.2±32.9 °C

Dorzolamide hydrochloride

Dorzolamide Hcl(L671152 Hcl; MK507 Hcl) is an anti-glaucoma agent, which is a carbonic anhydrase inhibitor.Target: carbonic anhydrase (CA)Dorzolamide hydrochloride is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour [1]. Glaucoma was induced in the right eye of adult Wistar rats by episcleral venous occlusion. One experimental group was administered dorzolamide hydrochloride 2%-timolol 0.5% combination eye drops, while the other experimental group was administered dorzolamide hydrochloride2% eye drops. Control groups had surgery without drug administration. Drug application was initiated either 2 weeks before surgery (Group A), from the day of surgery (Group B), 2 weeks after surgery (Group C), or 4 weeks after surgery (Group D). RGCs were labeled by intratectal Fluorogold injections and counted from flat-mount preparations, and IOP was measured using Tonopen. Both dorzolamide-timolol combination and dorzolamide hydrochloride, when applied topically, significantly reduced IOP and improved RGC densities in experimental eyes when compared to control eyes. Earlier initiation, as well as longer duration of drug application, resulted in higher RGC densities [2].Clinical indications: Glaucoma; Ocular hypertensionFDA Approved Date: 1995Toxicity: Dizziness, headache, shortness of breath, slow heartbeat, severe asthma, cardiac arrest

  • CAS Number: 130693-82-2
  • MF: C10H17ClN2O4S3
  • MW: 360.90100
  • Catalog: Carbonic Anhydrase
  • Density: 1.53 g/cm3
  • Boiling Point: 575.8ºC at 760 mmHg
  • Melting Point: 283-285ºC
  • Flash Point: 302ºC

Dorzolamide

Dorzolamide(L671152; MK507) is an anti-glaucoma agent, which is a carbonic anhydrase inhibitor.Target: carbonic anhydrase (CA)Dorzolamide is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour [1]. Glaucoma was induced in the right eye of adult Wistar rats by episcleral venous occlusion. One experimental group was administered dorzolamide 2%-timolol 0.5% combination eye drops, while the other experimental group was administered dorzolamide 2% eye drops. Control groups had surgery without drug administration. Drug application was initiated either 2 weeks before surgery (Group A), from the day of surgery (Group B), 2 weeks after surgery (Group C), or 4 weeks after surgery (Group D). RGCs were labeled by intratectal Fluorogold injections and counted from flat-mount preparations, and IOP was measured using Tonopen. Both dorzolamide-timolol combination and dorzolamide, when applied topically, significantly reduced IOP and improved RGC densities in experimental eyes when compared to control eyes. Earlier initiation, as well as longer duration of drug application, resulted in higher RGC densities [2].Clinical indications: Glaucoma; Ocular hypertensionFDA Approved Date: 1995Toxicity: Dizziness, headache, shortness of breath, slow heartbeat, severe asthma, cardiac arrest

  • CAS Number: 120279-96-1
  • MF: C10H16N2O4S3
  • MW: 324.44
  • Catalog: Carbonic Anhydrase
  • Density: 1.53 g/cm3
  • Boiling Point: 575.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 302ºC

Dimethylfraxetin

Dimethylfraxetin is a Carbonic anhydrase inhibitor, with a Ki value of 0.0097 μM.

  • CAS Number: 6035-49-0
  • MF: C12H12O5
  • MW: 236.221
  • Catalog: Carbonic Anhydrase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 408.0±45.0 °C at 760 mmHg
  • Melting Point: 104-105ºC
  • Flash Point: 184.3±28.8 °C