CB1 antagonist 4

SKU: orb1298869

Description

TM38837

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	1253641-65-4
MW	617.51
Purity	98.97%
Formula	C₃₀H₂₅Cl₂F₃N₄OS
SMILES	CCc1c(nn(c1-c1ccc(s1)C#Cc1ccc(cc1)C(F)(F)F)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1
Target	Cannabinoid Receptor
Solubility	10% DMSO+90% Corn Oil:4 mg/mL (6.48 mM);DMSO:40 mg/mL (64.78 mM)

Bioactivity

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In Vivo

CB1 antagonist 4, a novel, largely peripherally restricted CB1 antagonist, in terms of fear-promoting consequences of systemic vs. intracerebral injections.Different groups of male C57BL/6 N mice underwent auditory fear conditioning, followed by re-exposure to the tone.Mice were treated per os (p.o.) with CB1 antagonist 4 (10, 30, or 100 mg/kg), rimonabant (10 mg/kg;a brain penetrating CB1 antagonist/inverse agonist which served as a positive control), or vehicle, 2 h prior the tone presentation.Only the high dose of CB1 antagonist 4 (100 mg/kg) induced a significant increase in freezing behavior, similar to that induced by rimonabant (10 mg/kg) (p <0.001). If injected into the brain both CB1 antagonist 4 (10 or 30 μg/mouse) and rimonabant (1 or 10 μg/mouse) caused a sustained fear response to the tone, which was more pronounced after rimonabant treatment.Taken together, CB1 antagonist 4 was at least one order of magnitude less effective in promoting fear responses than rimonabant.Given the equipotency of the two CB1 antagonists with regard to weight loss and metabolic syndrome-like symptoms in rodent obesity models, our results point to a critical dose range in which CB1 antagonist 4 might be beneficial for indications such as obesity and metabolic disorders with limited risk of fear-promoting effects.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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CB, CB1, Cannabinoid Receptor, CannabinoidReceptor, antiobesity, metabolic, inhibit, fat, fear, Inhibitor, peripheral, TM 38837, TM38837, TM-38837

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Compound Identifiers

PubChem CID

49779607 ↗

Key Properties

−

No computed properties available.

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CB1 antagonist 4 (orb1298869)

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Formula:	C₁₇H₁₉Cl₂N₅O

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MW:	974.97
Formula:	C₅₆H₅₃Cl₂N₇O₅

Purity:	99.78%
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MW:	489.82
Formula:	C₂₄H₂₃Cl₃N₄O

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MW:	605.46
Formula:	C₂₅H₂₅Cl₂F₃N₄O₄S

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MW:	452.28
Formula:	C₂₁H₁₇Cl₂F₂N₃O₂

CB1 antagonist 4

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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CB1 antagonist 4 (orb1298869)

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