- Senicapoc
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- $0.00 / 10MG
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2024-09-15
- CAS:289656-45-7
- Min. Order: 10MG
- Purity: 99.0%min. HPLC
- Supply Ability: 10000
- Senicapoc
-
- $15.00 / 1KG
-
2021-07-13
- CAS:289656-45-7
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
- Senicapoc
-
- $15.00 / 1KG
-
2021-07-10
- CAS:289656-45-7
- Min. Order: 1KG
- Purity: 99%+ HPLC
- Supply Ability: Monthly supply of 1 ton
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| | Senicapoc Basic information |
| Product Name: | Senicapoc | | Synonyms: | 2,2-bis(4-fluorophenyl)-2-phenyl-acetamide;Benzeneacetamide, 4-fluoro-a-(4-fluorophenyl)-a-phenyl-;4-Fluoro-alpha-(4-fluorophenyl)-alpha-phenylbenzeneacetamide;4-Fluoro-A-(4-Fluorophenyl)-A-Phenyl-BenzeneacetaMide;ICA 17043;Senicapoc;ICA-17043;ICA 17043;ICA17043;Benzeneacetamide, 4-fluoro-α-(4-fluorophenyl)-α-phenyl- | | CAS: | 289656-45-7 | | MF: | C20H15F2NO | | MW: | 323.34 | | EINECS: | | | Product Categories: | | | Mol File: | 289656-45-7.mol |  |
| | Senicapoc Chemical Properties |
| Melting point | 180-181 °C(Solv: hexane (110-54-3); dichloromethane (75-09-2)) | | Boiling point | 460.7±45.0 °C(Predicted) | | density | 1.250±0.06 g/cm3(Predicted) | | storage temp. | Sealed in dry,Store in freezer, under -20°C | | solubility | DMSO : 50 mg/mL (154.64 mM; Need ultrasonic) | | form | Powder | | pka | 15.41±0.50(Predicted) | | color | White to yellow | | InChI | InChI=1S/C20H15F2NO/c21-17-10-6-15(7-11-17)20(19(23)24,14-4-2-1-3-5-14)16-8-12-18(22)13-9-16/h1-13H,(H2,23,24) | | InChIKey | SCTZUZTYRMOMKT-UHFFFAOYSA-N | | SMILES | C(C1C=CC=CC=1)(C1C=CC(F)=CC=1)(C1C=CC(F)=CC=1)C(=O)N |
| | Senicapoc Usage And Synthesis |
| Description | Senicapoc is an inhibitor of intermediate conductance calcium-activated potassium (IKCa1/KCa3.1) channels. It inhibits rubidium efflux from and dehydration of isolated human red blood cells (RBCs) induced by the calcium ionophore A23187 (; IC50s = 11 and 30 nM, respectively). Senicapoc (10 mg/kg twice per day) reduces IKCa1/KCa3.1 channel activity, increases potassium levels in RBCs, and decreases erythrocyte density in the SAD transgenic mouse model of sickle cell disease. It inhibits IL-2, IFN-γ, IL-12, and IL-17A production in CD3+ T cells stimulated with phorbol 12-myristate 13-acetate (PMA; ) and ionomycin (Item Nos. 10004974 | 11932) when used at a concentration of 1 μM. Senicapoc (100 mg/kg) increases the paw withdrawal threshold in a rat model of chronic constriction injury (CCI) of the sciatic nerve. | | Uses | Treatment of disorders mediated by a calcium activated intermediate conductance potassium ion channel antagonist. | | Definition |
Senicapoc (ICA-17043; bis(4-fluorophenyl)phenyl acetamide), a selective, highly potent Gardos channel blocker (IC50 = 11 nM), specifically inhibits the efflux of potassium from the RBCs of both SCD transgenic mice and human sickle cell disease patients. It is derived from clotrimazole-1, a KCNN4 inhibitor. Senicapoc is well tolerated by both healthy volunteers and patients with SCD and has favourable pharmacokinetics, with a long half-life permitting once-daily dosing. It was designed for long-term sickle cell disease therapy to avoid clotrimazole-1 side effects. Whereas Senicapoc is a potent inhibitor of WT KCNN4, its efficiency on mutated channels was unknown[1-2].
| | References |
[1] Raphael Rapetti-Mauss. “Senicapoc: a potent candidate for the treatment of a subset of hereditary xerocytosis caused by mutations in the Gardos channel.” Haematologica 101 11 (2016): e431–e435.
[2] Kenneth I Ataga. “Efficacy and safety of the Gardos channel blocker, senicapoc (ICA-17043), in patients with sickle cell anemia.” Blood (2008): 3991–7.
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| | Senicapoc Preparation Products And Raw materials |
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