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Chemical Structure : ZYKR1
Catalog No.: PC-21574Not For Human Use, Lab Use Only.
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).
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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.
| M.Wt | 811.98 | |
| Formula | C41H61N7O10 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jain MR, et al. Eur J Pharmacol. 2022 Jun 5;924:174961.
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