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[CAS NO. 1163-36-6] Clemizolehydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-30234A |
| Brand: | MCE |
| CAS: | 1163-36-6 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 362.30 |
| Molecular Formula | C19H21Cl2N3 |
| SMILES | ClC1=CC=C(C=C1)CN2C(CN3CCCC3)=NC4=CC=CC=C24.[H]Cl |
Summary
Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole hydrochloride is an inhibitor of TRPC5 channel . The IC 50 of Clemizole hydrochloride for RNA binding by NS4B is 24 nM, whereas its EC 50 for viral replication is 8 µM.
In Vitro
Clemizole hydrochloride is found to inhibit HCV RNA replication in cell culture that is mediated by its suppression of NS4B’s RNA binding, with little toxicity for the host cell. The EC 50 of Clemizole on the W55R mutant J6/JFH RNA is ~18 µM (2.25 times the EC 50 of the wild-type RNA) [1] . Clemizole is a novel inhibitor of TRPC5 channels. Clemizole efficiently blocks TRPC5 currents and Ca 2+ entry in the low micromolar range (IC 50 =1.0-1.3 µM). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC 50 =6.4 µM), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC 50 =9.1 µM) and TRPC6 (IC 50 =11.3 µM). Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1 µM. The concentration-response curves confirmed a concentration-dependent block of TRPC5 by Clemizole and revealed an apparent IC 50 of 1.1±0.04 µM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Clemizole hydrochloride has an unexpectedly short plasma half-life (measured at 0.15 hours); it is very rapidly biotransformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03069508 | Eiger Group International, Inc. |
Hepatocellular Carcinoma
|
February 13, 2017 | Phase 2 |
| NCT05066217 | Epygenix |
Lennox Gastaut Syndrome
|
October 1, 2022 | Phase 2 |
| NCT00945880 | Eiger BioPharmaceuticals |
Hepatitis C
|
July 2009 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 33.33 mg/mL ( 92.00 mM ; Need ultrasonic)
H 2 O : 20 mg/mL ( 55.20 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7601 mL | 13.8007 mL | 27.6014 mL |
| 5 mM | 0.5520 mL | 2.7601 mL | 5.5203 mL |
| 10 mM | 0.2760 mL | 1.3801 mL | 2.7601 mL |
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1.
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2.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution
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3.
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4.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.74 mM); Clear solution
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5.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.74 mM); Clear solution
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6.
Add each solvent one by one: 1% DMSO >> 99% saline
Solubility: 0.5 mg/mL (1.38 mM); Clear solution; Need ultrasonic
References
- [1] Einav S, et al. Discovery of a hepatitis C target and its pharmacological inhibitors by microfluidic affinity analysis. Nat Biotechnol. 2008 Sep;26(9):1019-27
- [2] Richter JM, et al. Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5. Mol Pharmacol. 2014 Nov;86(5):514-21
- [3] Nishimura T, et al. Using chimeric mice with humanized livers to predict human drug metabolism and a drug-drug interaction. J Pharmacol Exp Ther. 2013 Feb;344(2):388-96.
Synonyms
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