CLP257

CLP257 is a selective K+-Cl− cotransporter KCC2 activator (EC50: 616 nM) and it is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 alleviates hypersensitivity in rats with neuropathic painc and it also modulates plasmalemmal KCC2 protein turnover post-translationally. CLP257 restores impaired Cl− transport in neurons with diminished KCC2 activity.

Catalog No. T14984Cas No. 1181081-71-9

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Purity:98.13%

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CLP257

Catalog No. T14984Cas No. 1181081-71-9

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Pack Size	Price	Availability
1 mg	$38	In Stock
2 mg	$54	In Stock
5 mg	$89	In Stock
10 mg	$143	In Stock
25 mg	$298	In Stock
50 mg	$490	In Stock
100 mg	$723	In Stock

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Product Introduction

Bioactivity

Description	CLP257 is a selective K+-Cl− cotransporter KCC2 activator (EC50: 616 nM) and it is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 alleviates hypersensitivity in rats with neuropathic painc and it also modulates plasmalemmal KCC2 protein turnover post-translationally. CLP257 restores impaired Cl− transport in neurons with diminished KCC2 activity.
Targets&IC50	KCC2:（EC50）616 nM
In vitro	Oocyte pre-incubation with CLP257 (200 nM) increases KCC2 transport activity by 61%. However, it causes no change in other CCCs. There is no change in [Cl?]i in HEK293-cl cells when incubated with CLP257. CLP257 (50 μM) provokes < 0.2% of the effect of 5 μM muscimol in CHO cells transduced with recombinant α1β2γ2 GABAA receptors. Dose-dependent antagonism is also observed between CLP257 and the recently characterized KCC2 antagonist VU024055119 [1].
In vivo	CLP257 (100?mg/kg; i.p.; adult male rats) treatment causes an obvious increase in mechanical sensitivity [2].

Chemical Properties

Molecular Weight	307.34
Formula	C₁₄H₁₄FN₃O₂S
Cas No.	1181081-71-9

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

Solubility Information

DMSO: 17.86 mg/mL (58.11 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2537 mL	16.2686 mL	32.5373 mL	162.6863 mL
5 mM	0.6507 mL	3.2537 mL	6.5075 mL	32.5373 mL
10 mM	0.3254 mL	1.6269 mL	3.2537 mL	16.2686 mL
20 mM	0.1627 mL	0.8134 mL	1.6269 mL	8.1343 mL
50 mM	0.0651 mL	0.3254 mL	0.6507 mL	3.2537 mL

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