1. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel PI3K/Akt/mTOR
  2. Carbonic Anhydrase NKCC mTOR
  3. CAII/VII-IN-1

CAII/VII-IN-1 是一种口服活性的 hCA II (KI = 12.3 nM) 和 hCA VII (KI = 22.6 nM) 抑制剂,对 hCA I 没有表现出明显的活性。CAII/VII-IN-1 在体内Pilocarpine (HY-B0726A) 诱发的癫痫模型中表现出优异的神经保护活性。CAII/VII-IN-1 可以上调 KCC2 并抑制 mTOR,发挥神经保护作用。CAII/VII-IN-1 没有表现出任何明显的神经毒性作用或肝肾功能的改变。CAII/VII-IN-1 可用于癫痫的研究。

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CAII/VII-IN-1

CAII/VII-IN-1 Chemical Structure

CAS No. : 3085155-69-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CAII/VII-IN-1 is an orally active hCA II (KI = 12.3 nM), and hCA VII (KI = 22.6 nM) inhibitor, showing no significant activity against hCA I. CAII/VII-IN-1 shows excellent neuroprotective activity in vivo Pilocarpine (HY-B0726A)-induced seizure model. CAII/VII-IN-1 can upregulate KCC2 and inhibit mTOR, exerting neuroprotective effects. CAII/VII-IN-1 does not show any significant neurotoxic effects or alterations in liver and kidney function. CAII/VII-IN-1 can be used for the study of epilepsy[1].

体外研究
(In Vitro)

CAII/VII-IN-1 (Compound 16d) 在 Vero 细胞中在给定浓度下是安全的 (IC50 = 59.7 μM)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CAII/VII-IN-1(200 mg/kg,口服,一次)在 Pilocarpine 诱导的小鼠中产生明显的抗惊厥和抗癫痫作用,表现为癫痫发作潜伏期增加两倍,癫痫发作严重程度显着降低,海马稳态恢复[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male mice (20-25 g) were injected with Pilocarpine[1].
Dosage: Orally before Pilocarpine injection.
Administration: Delayed seizures by more than twice as long as the Pilocarpine group (108.6 %).
Result: Delayed seizures by more than twice as long as the Pilocarpine group (108.6 %).
Showed comparable efficacy in delaying seizure onset and reducing severity at most time points.
Reached 100 % survival.
Upregulated KCC2 (188.1%) and inhibited mTOR (51.39%) exert neuroprotective effects.
分子量

639.11

Formula

C27H23ClN8O5S2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CAII/VII-IN-1
目录号:
HY-178362
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