MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

SKA-121

CAS No. : 1820708-73-3

MCE 国际站：SKA-121

产品活性：SKA-121 是一种选择性的 K_Ca3.1 激活剂。SKA-121 作用于 K_Ca3.1 和 K_Ca2.3，EC₅₀ 分别为 109 nM 和 4.4 μM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Potassium Channel

In Vitro: SKA-121, a compound generated through an isosteric replacement approach. SKA-121 is a typical positive-gating modulator and shifts the calcium-concentration response curve of K_Ca3.1 to the left. SKA-121 displays 41-fold selectivity for K_Ca3.1 (EC₅₀ 109 nM±14 nM) over K_Ca2.3 (EC₅₀ 4.4 ± 1.6 μM). SKA-121 is 200- to 400-fold selective over representative K_V (K_V1.3, K_V2.1, K_V3.1, and K_V11.1), Na_V (Na_V1.2, Na_V1.4, Na_V1.5, and NaV1.7), as well as Ca_V1.2 channels.

In Vivo: In blood pressure telemetry experiments, SKA-121 (100 mg/kg i.p.) significantly lowers mean arterial blood pressure in normotensive and hypertensive wild-type but not in K_Ca3.1^-/- mice. SKA-121 can be used as a new K_Ca3.1 selective pharmacological tool compound despite its relatively short half-life in mice. A lower dose of 30 mg/kg of SKA-121 does not produce significant alterations in MAP. The vehicle, peanut oil/DMSO (9:1 v/v, for SKA-121), does not cause significant alterations in MAP or HR. SKA-121 has a short half-life (~20 minutes), and plasma decay is extremely rapid (21.3±2.4 μM at 5 minutes; 483±231 nM at 1 hour and 53±44 nM at 4 hours). Since SKA-121 is relatively well soluble (logP=1.79) and can potentially be added to drinking water in animal experiments, it orally is also administered, and find that it has an oral availability of roughly 25%.

相关产品：Bioactive Compound Library Plus  |  Membrane Transporter/Ion Channel Compound Library  |  Anti-Cardiovascular Disease Compound Library  |  Neuroprotective Compound Library  |  Targeted Diversity Library  |  Potassium Channel Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Activators Library  |  Mitiglinide-d₅ calcium  |  Ropivacaine hydrochloride  |  WX-081  |  Doxapram hydrochloride hydrate  |  TASK-1-IN-1  |  VU0134992  |  BL-1249  |  Dendrotoxin K  |  Disopyramide  |  Domiphen bromide  |  Dehydrosoyasaponin I  |  20(S)-Ginsenoside Rg3  |  (Rac)-Ropivacaine-d₇  |  AZD-5672  |  Daurisoline  |  (+)-KCC2 blocker 1  |  ML252  |  Ketanserin  |  Ropivacaine mesylate  |  AMP-PNP tetralithium  |  PK-THPP  |  Ifenprodil tartrate  |  DDO-02005  |  Hydrochlorothiazide-¹³C₆  |  Brompheniramine maleate  |  Meclofenamic acid sodium hydrate  |  DMP-543  |  BAPTA-AM  |  PNU 37883 hydrochloride  |  Quinine hydrochloride dihydrate

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

货号: HY-107414

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。