[CAS NO. 1181081-71-9] CLP257
PRODUCTS SPECIFICATIONS [1181081-71-9]
DESCRIPTION [1181081-71-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 307.34 |
| Molecular Formula | C14H14FN3O2S |
| SMILES | O=C1N=C(N2CCCCN2)S/C1=C\C3=CC=C(F)C=C3O |
Summary
CLP257 is a selective K + -Cl − cotransporter KCC2 activator with an EC 50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl − transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally [1] [2] .
IC50 & Target
EC50: 616 nM (KCC2) [1]
In Vitro
There is no change in [Cl − ] i in HEK293-cl cells when incubated with CLP257, indicating inactivity on NKCC1, KCC1, KCC3 or KCC4. Oocyte pre-incubation with CLP257 (200 nM) increases KCC2 transport activity by 61%, but causes no change in other CCCs. Functional, dose-dependent antagonism is also observed between CLP257 and the recently characterized KCC2 antagonist VU024055119. CLP257 (50 μM) provokes < 0.2% of the effect of 5 μM muscimol in CHO cells transduced with recombinant α1β2γ2 GABAA receptors, indicating negligible agonist activity of CLP257 on GABAA receptors [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CLP257 (100 mg/kg; intraperitoneal injection; adult male rats) treatment induced a significant increase in mechanical sensitivity [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Adult male rats (300 g) injected with Morphine [2] |
| Dosage: | 100 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Induced a significant increase in mechanical sensitivity. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years |
* The compound is unstable in solutions, freshly prepared is recommended.
Solvent & Solubility
DMSO : 17.86 mg/mL ( 58.11 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.2537 mL | 16.2686 mL | 32.5373 mL |
| 5 mM | 0.6507 mL | 3.2537 mL | 6.5075 mL |
| 10 mM | 0.3254 mL | 1.6269 mL | 3.2537 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: 1.79 mg/mL (5.82 mM); Clear solution; Need ultrasonic
References
