标签归档：pg

PG-931

发表于由

PG-931;

PG-931 是 SHU 9119 (HY-P0227) 的类似物。PG-931 是一种强效的黑素皮质素 4 (MC4) 受体 (IC50=0.58 nM) 激动剂，比 hMC3R (IC50=55 nM) 或 hMC5R (IC50=2.4 nM) 更具选择性。PG-931 在动物实验模型中，可逆转出血休克，防止体内多器官损伤。

PG-931amp;;

PG-931 Chemical Structure

CAS No. : 667430-81-1

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生物活性

PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo[2].

IC50 Target

IC50: 0.58 nM (melanocortin 4 receptor)
IC50: 2.4 nM (melanocortin 5 receptor)
IC50: 55 nM (melanocortin 3 receptor)[1]
体内研究
(In Vivo)

PG-931 (intravenous injection; 13-108 nmol/kg; single dose) produces a dose-dependent restoration of cardiovascular and respiratory functions, and improved survival in Wistar rats with haemorrhagic shock[2].

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

Animal Model: Wistar rats[2]
Dosage: 13-108 nmol/kg
Administration: Intravenous injection; single dose
Result: Exhibitd an anti-shock effect occurred at nanomolar doses.

分子量

1180.40

Formula

C59H85N15O11
CAS 号

667430-81-1
Sequence Shortening

Ac-{Nle}-DP-{D-Phe}-RWKPV-NH2 (Lactam bridge:Asp2-Lys7)
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.
参考文献

  • [1]. D Giuliani, et al. Selective melanocortin MC4 receptor agonists reverse haemorrhagic shock and prevent multiple organ damage. Br J Pharmacol

    [2]. P Grieco, et al. Extensive structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. J Pept Res

PG106

发表于由

PG106;

PG106 是一种有效的、选择性的 hMC3 receptor 拮抗剂 (IC50= 210 nM)，对 hMC4 受体(EC50=9900 nM) 和 hMC5 受体无活性。

PG106amp;;

PG106 Chemical Structure

CAS No. : 944111-22-2

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PG106 的其他形式现货产品:

PG106 TFA

生物活性

PG106 is a potent and selective human melanocortin 3 (hMC3) receptor antagonist (IC50=210 nM) and has noactivity at hMC4 receptors (EC50=9900 nM) and hMC5 receptor[1].

IC50 Target

IC50: 210 nM (hMC3 receptor)
EC50: 9900 nM (hMC4 receptor)[1]
分子量

1008.18

Formula

C51H69N13O9
CAS 号

944111-22-2
Sequence Shortening

Ac-{Nle}-D-{Bal}-{D-Nal}-RWK-NH2 (Lactam bridge:Asp2-Lys7)
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.
参考文献

  • [1]. Paolo Grieco, et al. Further structure-activity studies of lactam derivatives of MT-II and SHU-9119: their activity and selectivity at human melanocortin receptors 3, 4, and 5. Peptides