JTC-801 HCl
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $459 | Check With Us |
500mg | $750 | Check With Us |
1g | $1125 | Check With Us |
Cat #: V1275 CAS #: 244218-51-7 Purity ≥ 98%
Description: JTC-801 HCl (JTC 801; JTC801), the hydrochloride salt of JTC801, is a potent, orally bioactive and selective opioid receptor-like1 (ORL1) receptor antagonist with potential analgesic activity.
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Molecular Weight (MW) | 447.96 |
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Molecular Formula | C26H25N3O2.HCl |
CAS No. | 244218-51-7 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 90 mg/mL (200.9 mM)r |
Water: < 1 mg/mLr | |
Ethanol: 31 mg/mL (69.2 mM) | |
Solubility In Vivo | 0.5% methylcellulose: 30 mg/mL |
Synonyms | JTC-801; JTC 801; JTC801 HCl |
Protocol | 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 |
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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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.2323 mL | 11.1617 mL | 22.3234 mL | 44.6468 mL |
5mM | 0.4465 mL | 2.2323 mL | 4.4647 mL | 8.9294 mL |
10mM | 0.2232 mL | 1.1162 mL | 2.2323 mL | 4.4647 mL |
20mM | 0.1116 mL | 0.5581 mL | 1.1162 mL | 2.2323 mL |
The molarity calculator equation
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The dilution calculator equation
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.