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JTC-801

Cat. No. M2214
JTC-801 Structure
Size Price Availability Quantity
10mg USD 83  USD83 In stock
25mg USD 165  USD165 In stock
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Quality Control & Documentation
Biological Activity

JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor with a Ki of 8.2 nM. JTC-801 inhibited the binding of [(3)H]-nociceptin to human ORL(1) receptors expressed in HeLa cells with a K(i) value of 44.5 nM. JTC-801 (1 mg/kg, i.p.) blocked a significant proportion of the hypothermia caused by each dose of WIN 55212-2 (2.5, 5, and 10 mg/kg, i.p.). JTC-801 (1 mg/kg, i.p.) also blocked the hypothermia caused by another cannabinoid agonist, CP-55940 (1 mg/kg, i.p.). JTC-801 exhibits anti-nociceptive effects in acute pain models in vivo. JTC-801 reduced both the first and second phases of the nociceptive response with MED of 0.01 mg kg(-1) by i.v. administration or 1 mg kg(-1) by p.o. administration in the rat formalin test.

Chemical Information
Molecular Weight 447.96
Formula C26H25N3O2.HCl
CAS Number 244218-51-7
Solubility (25°C) DMSO 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Rawls SM, et al. Neuropeptides. NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats.

[2] Tamai H, et al. Eur J Pharmacol. Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation.

[3] Yamada H, et al. Br J Pharmacol. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801.

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