A selective inverse agonist of peripheral CB1 receptors
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JD5037

Item No. 12053

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2S-[[[(4S)-3-(4-chlorophenyl)-4,5-dihydro-4-phenyl-1H-pyrazol-1-yl][[(4-chlorophenyl)sulfonyl]amino]methylene]amino]-3-methyl-butanamide
CAS Number
1392116-14-1
Molecular Formula
C27H27Cl2N5O3S
Formula Weight
572.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 25 mg/ml
λmax
227, 315 nm
SMILES
ClC(C=C1)=CC=C1C2=NN(/C(N[C@@H](C(C)C)C(N)=O)=N/S(C3=CC=C(Cl)C=C3)(=O)=O)C[C@@H]2C4=CC=CC=C4
InChi Code
InChI=1S/C27H27Cl2N5O3S/c1-17(2)24(26(30)35)31-27(33-38(36,37)22-14-12-21(29)13-15-22)34-16-23(18-6-4-3-5-7-18)25(32-34)19-8-10-20(28)11-9-19/h3-15,17,23-24H,16H2,1-2H3,(H2,30,35)(H,31,33)/t23-,24+/m1/s1
InChi Key
GTCSIQFTNPTSLO-RPWUZVMVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $28

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    5 mg

    $104

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    10 mg

    $165

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    25 mg

    $275

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    JD5037 is an inverse agonist of peripheral cannabinoid 1 (CB1) receptors (Ki = 0.35 nM).1 It displays >700-fold selectivity for CB1 over CB2, >1,000-fold selectivity over a panel of 70 receptors, transporters, and ion channels, and low blood-brain barrier penetrance.1,2 JD5037 is orally bioavailable and reduces food intake, body weight, and hormonal/metabolic abnormalities in diet-induced obese mice.1,3 JD5037 reverses hyperphagia, reduces body weight, and improves metabolic parameters in Magel2-null mice, a model of Prader-Willi syndrome.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tam, J., Cinar, R., Liu, J., et al. Peripheral cannabinoid-1 receptor inverse agonism reduces obesity by reversing leptin resistance. Cell Metab. 16(2), 167-179 (2012).

    2. Chorvat, R.J., Berbaum, J., Seriacki, K., et al. JD-5006 and JD-5037: Peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities. Bioorg. Med. Chem. Lett. 22(19), 6173-6180 (2012).

    3. Cinar, R., Godlewski, G., Liu, J., et al. Hepatic cannabinoid-1 receptors mediate diet-induced insulin resistance by increasing de novo synthesis of long-chain ceramides. Hepatology 59(1), 143-153 (2014).

    4. Knani, I., Earley, B.J., Udi, S., et al. Targeting the endocannabinoid/CB1 receptor system for treating obesity in Prader-Willi syndrome. Mol. Metab. 5(12), 1187-1199 (2016).