>>Signaling Pathways>> Membrane Transporter/Ion Channel>> Calcium Channel>>NS-638

NS-638

Catalog No.GC30997

NS-638은 Ca2+-채널 차단 특성을 가진 작은 비펩티드 분자입니다.

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NS-638 Chemical Structure

Cas No.: 150493-34-8

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$83.00
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5mg
US$88.00
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10mg
US$130.00
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50mg
US$436.00
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100mg
US$593.00
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Sample solution is provided at 25 µL, 10mM.

Description of NS-638

NS-638 is a small nonpeptide molecule with Ca2+-channel blocking properties. K+-stimulated intracellular Ca2+-elevation is blocked with an IC50 value of 3.4 μM.

NS-638 dose dependently inhibits K+-stimulated [45 Ca2+]-uptake in chick cortical synaptosomes and 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA)- stimulated [3H]GABA-release from cultured cortical neurons with IC50 values of 2.3 and 4.3 μM, respectively. K+-stimulated intracellular Ca2+-elevation in cultured cerebellar granule cells is equipotently blocked with an IC50 value of 3.4 μM. At this concentration no effect on Ca2+-induced contractions in K+-depolarized guinea pig taenia coli is observed. NS-638 reversibly blocks N- and L-type Ca2+-channels in cultured chick dorsal root ganglion cells in the concentration range of 1-30 μM[1].

In the mouse middle cerebral artery occlusion model, NS-638 administered i.p. (50 mg kg-1) at 1 h and 6 h post-ischemia, and once a day for the next two days, results in a 48% reduction in total infarct volume. It does not show protection against ischemic neuronal damage in the gerbil model of bilateral carotid artery occlusion[1].

[1]. M?ller A, et al. Pharmacological profile and anti-ischemic properties of the Ca(2+)-channel blocker NS-638. Neurol Res. 1995 Oct;17(5):353-60.

Protocol of NS-638

Cell experiment:

The effect of NS-638 on neuronal Ca2+-channels is evaluated using whole cell patch clamp techniques[1].

Animal experiment:

Mice: In the mouse middle cerebral artery occlusion model, NS-638 is administered i.p. (50 mg kg-1) at 1 h and 6 h post-ischemia, and once a day for the next two days[1].

References:

[1]. Møller A, et al. Pharmacological profile and anti-ischemic properties of the Ca(2+)-channel blocker NS-638. Neurol Res. 1995 Oct;17(5):353-60.

Chemical Properties of NS-638

Cas No. 150493-34-8 SDF
Canonical SMILES NC1=NC2=CC(C(F)(F)F)=CC=C2N1CC3=CC=C(Cl)C=C3
Formula C15H11ClF3N3 M.Wt 325.72
Solubility DMSO : ≥ 34 mg/mL (104.38 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of NS-638

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.0701 mL 15.3506 mL 30.7012 mL
5 mM 0.614 mL 3.0701 mL 6.1402 mL
10 mM 0.307 mL 1.5351 mL 3.0701 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Review for NS-638

Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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