Size | Price | Stock |
---|---|---|
5mg | $50 | In-stock |
10mg | $80 | In-stock |
50mg | $330 | In-stock |
100 mg | Get quote | |
200 mg | Get quote | |
We match the lowest price on market. |
We offer a substantial discount on larger orders, please inquire via [email protected]
or Fax: (86)21-58955996
Inquiry for price and availability only. Please place your order via our email or fax.
Cat. No. : | HY-13274 |
M.Wt: | 447.96 |
Formula: | C26H26ClN3O2 |
Purity: | >98 % |
Solubility: | DMSO : 100 mg/mL (223.23 mM; Need ultrasonic); H2O : ≥ 0.33 mg/mL (0.74 mM) |
JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM. IC50 & Target: Ki: 8.2 nM (ORL1)[2] In Vitro: JTC-801 inhibits [3H]-nociceptin binding to ORL1 receptor expressed in HeLa cells with an IC50 value of 94±8.6 nm at a [3H]-nociceptin concentration of 50 pM. JTC-801 weakly inhibits the binding of the ligands to human δ receptor (IC50>10 μM), κ receptor (IC50>10 μM), and μ receptor (IC50=325 nM). In rat cerebrocortical membrane, JTC-801 inhibits ORL1 receptor (IC50=472 nM) and μ receptor (IC50=1831 nM). JTC-801 at a concentration of 10 μM reverses the inhibitory action of nociceptin against forskolin-induced increase in cyclic AMP level (IC50: 2.58 μM, 1 nM of nociceptin used). JTC-801 alone does not affect the the production of cyclic AMP[1]. The affinity of JTC-801 for ORL1 receptor, human opioid μ-, κ-, and δ-receptors is 8.2 nM, 102.9 nM, 1057.5 nM and 8647.2 nM[2]. In Vivo: JTC-801 (≥0.01 mg/kg, i.v. or 1 mg/kg, p.o.) antagonizes the nociceptin-induced allodynia in mice. In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL) to exposed heat stimulus with minimum effective doses (MED) of 0.01 mg/kg by i.v. or 1 mg/kg by p.o. In the rat formalin test, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01 mg/kg by i.v. administration or 1 mg/kg by p.o. administration. This anti-nociceptive action of JTC-801 is not inhibited by naloxone (10 mg/kg, s.c.). JTC-801 antagonizes the ORL1 receptor response, and has efficacious and potent anti-nociceptive effects in acute pain animal models not only by intravenous injection but also oral administration[1]. JTC-801 (0.3 mg/kg) decreases allodynia induced by the intrathecal injection of nociceptin in mice[2]. JTC-801 (6 mg/kg i.p., once daily) reverses SPS-induced mechanical allodynia, thermal hyperalgesia, anxiety-like behaviour and hypocortisolism. JTC-801 treatment also reverses NOP receptor protein and mRNA up-regulation in amygdala and PAG. JTC-801 blocks elevated N/OFQ levels in serum, CSF, PAG and hippocampus at day 21 of SPS[3]. JTC-801 (0.05-5 mg/kg, i.p.) supresses the the analgesic effect of N2O in 129Sv mice by the writhing test and tail flick test[4].
Lorem ipsum dolor sit amet, consectetur adipisicing elit. Autem earum hic iste maiores, nam neque rem suscipit. Adipisci consequatur error exercitationem fugit ipsam optio qui, quibusdam repellendus sed vero! Debitis.
Inquiry Information
Your information is safe with us.