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Cat. No. M2214
JTC-801 Structure
Size Price Availability Quantity
10mg USD 70  USD70 In stock
50mg USD 280  USD280 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 447.96
Formula C26H25N3O2.HCl
CAS Number 244218-51-7
Purity >98%
Solubility DMSO 80 mg/mL
Storage at -20°C

[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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Keywords: JTC-801 supplier, Opioid Receptor, inhibitors

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