JD-5037 is a cannabinoid-1 receptor blocker (CB1R antagonist) with IC50 of 1.5 nM. JD-5037 is very selective for the CB1 subtype, with a Ki of 0.35nM, >700-fold higher affinity than it has for CB2 receptors. In vivo, JD5037 (3 mg/kg/d, i.p.) induces equal reductions in body weight, attenuates the HFD-induced hyperglycemia, and reduces the HFD-induced hepatic injury and steatosis in obese Magel2-null mice. JD5037 (3 mg/kg/day, p.o.) significantly reduces the size of tumors and abrogates the tumor in DEN-treated mice.
| Molecular Weight | 572.51 |
| Formula | C27H27Cl2N5O3S |
| CAS Number | 1392116-14-1 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Robert J Chorvat, et al. Bioorg Med Chem Lett. Peripherally restricted CB1 receptor blockers
| Related Cannabinoid Products |
|---|
| Vicasinabin
Vicasinabin (RG7774) is the potent agonist of cannabinoid receptor 2 (CB2). |
| INV-347
INV-347 is a CB1R inverse agonist that can be used in studies related to obesity. |
| RVD-Hpα TFA
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. |
| Hemopressin(human, mouse) TFA
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. |
| Hemopressin(rat) TFA
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
