| Bioactivity | KCC2 blocker 1 is an orally active and selective K+-Cl- cotransporter KCC2 blocker with an IC50 of 1 μM. KCC2 blocker 1 is a benzyl prolinate[1]. | ||||||||||||
| Target | IC50: 1 μM (KCC2) | ||||||||||||
| Invitro | KCC2 blocker 1 (compound 13; 100 μM) inhibits NKCC1 with 35%. | ||||||||||||
| In Vivo | KCC2 blocker 1 (compound 13; 1 mg/kg iv and 6 mg/kg po) has a t1/2 of 0.3 hours, a CL of 26 mL/min/kg, a C max of 457 ng/mL and a AUC of 726 ng•h/mL for male Wistar rats[1]. Animal Model: | ||||||||||||
| Name | KCC2 blocker 1 | ||||||||||||
| CAS | 1228439-36-8 | ||||||||||||
| Formula | C22H25NO5S | ||||||||||||
| Molar Mass | 415.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Pégurier C, et al. Benzyl prolinate derivatives as novel selective KCC2 blockers. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2542-5. |
KCC2 blocker 1
CAS: 1228439-36-8 F: C22H25NO5S W: 415.50
KCC2 blocker 1 is an orally active and selective K+-Cl- cotransporter KCC2 blocker with an IC50 of 1 μM. KCC2 blocker 1
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