Product Details
| Product Name:
CLP257 |
CAS No.:
1181081-71-9 |
| Purity:
98.13% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | CLP257 |
| 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. |
| 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]. |
| 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.
|
| Keywords | Inhibitor | post-translationally | hypersensitivity | plasma | Potassium Channel | neuropathic | antihyperalgesic | CLP-257 | CLP 257 | membrane | KcsA | mechanical | sensitivity | KCC2 | CLP257 | inhibit |
| Inhibitors Related | Minoxidil sulfate | Quinine | (±)-Naringenin | Tolbutamide | Tetraethylammonium bromide | Halothane | Butamben | Tetraethylammonium chloride | Cloperastine hydrochloride | 2,2,2-Trichloroethanol | Chlorzoxazone | Indapamide |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States