ZYKR1 | KOR agonist | Probechem Biochemicals

Chemical Structure : ZYKR1

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ZYKR1 (ZYKR1 diacetate)

货号: PC-21574Not For Human Use, Lab Use Only.

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1 g		Get quote

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生物&药学活性

ZYKR1 is a potent, and peripherally restricted kappa opioid receptor (KOR)-selective agonist with EC50 of 0.061 nM in cAMP assays, highly selective over the mu and delta opioid receptors (EC50>10 μM).
ZYKR1 does not bind mu, delta opioid, and NOP receptors in radioligand binding assays.
ZYKR1 produced concentration-dependent inhibition of electrically evoked contractions in isolated mouse vas deferens with an IC50 of 1.6 nM.
ZYKR1 showed peripheral restriction and potent analgesic efficacy in various in-vivo animal models (acetic acid induced visceral pain mouse model, ED50: 0.025 mg/kg, IV; ovariohysterectomy induced postoperative pain rat model, ED50: 0.023 mg/kg, IV; and C48/80 induced pruritus mouse model, ED50: 0.063 mg/kg, IV).
ZYKR1 has potent antinociceptive action in visceral pain and pruritus with limited CNS side effects in preclinical models.

物理化学性质&存储条件

分子量	811.98
分子式	C41H61N7O10
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(6-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)acetic acid compound with acetic acid (1:2)

参考文献

1. Jain MR, et al. Eur J Pharmacol. 2022 Jun 5;924:174961.

ZYKR1 (ZYKR1 diacetate)

生物&药学活性

物理化学性质&存储条件

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ZYKR1 (ZYKR1 diacetate)

生物&药学活性

物理化学性质&存储条件

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