1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. SX-3228

SX-3228 是一种选择性苯二氮卓类 (benzodiazepine1BZ1) 受体激动剂,IC50 为 17 nM。

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SX-3228 Chemical Structure

SX-3228 Chemical Structure

CAS No. : 156364-04-4

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  • 生物活性

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生物活性

SX-3228 is a selective benzodiazepine1 (BZ1) receptor agonist with an IC50 of 17 nM.

IC50 & Target

IC50: 17 nM (BZ1 receptor)[1]

体外研究
(In Vitro)

SX-3228 is a selective ligand for the BZ1 receptor. Among the BZ-receptor subtypes, SX-3228 preferentially binds to the BZ1 receptor (IC50=17 nM). It has very weak affinity for the BZ2 receptor (spinal cord: IC50=127 nM), and virtually no affinity for the peripheral type BZ receptor (kidney: IC50>10000 nM). A compound with similar selectivity, SX-3228 has been shown to bind to BZ receptors, but not to dopamine (D1, D2), serotonin (5-HT1, 5-HT2 and 5-HT3 subtypes), noradrenaline (α1, α2, β), GABA or acetylcholine (muscarinic) subtypes[1].

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

体内研究
(In Vivo)

Administration of 0.5-2.5 mg/kg SX-3228 to rats during the light phase induces a significant reduction of rapid-eye-movement sleep (REMS) (P<0.05) during the third recording hour. Administration of SX-3228 (0.5-2.5 mg/kg) at the beginning of the dark period significantly and dose-dependently reduces waking (W) and increases slow wave sleep (SWS) during the 6-h recording period (P<0.05-0.01); however, significant changes during the last recording hour are restricted to the 2.5 mg/kg dose (P<0.01)[1].

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

分子量

338.36

Formula

C18H18N4O3

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
Animal Administration
[1]

Rats[1]
Twelve male Wistar rats (350-380 g) are used. Subcutaneous (sc) injections are given in a final volume of 1.0 mL/kg. All rats are given the corresponding volume of control solution (saline+Tween-80) in the control sessions. Following sc injection, a 6-h sleep recording is started at approximately 8:00 a.m. At least 4 days are allowed to elapse between injections to avoid long-lasting and rebound effects on sleep. The effects of SX-3228 0.5-2.5 mg/kg are studied in one group of animals (N=6) during the light phase of the 12-h light:12-h dark cycle, starting 1 h after the beginning of the light period. Polysomnographic recordings are started immediately after control solution or drug administration. Each rat receives all four treatments (control, and 0.5, 1.0, 2.5 mg/kg SX-3228).

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

参考文献
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The molarity calculator equation

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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:
SX-3228
目录号:
HY-100291
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