1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. TRP Channel
  3. TRPV1 antagonist 3

TRPV1 antagonist 3 

Cat. No.: HY-144372 Purity: 99.30%
COA Handling Instructions

TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.

For research use only. We do not sell to patients.

TRPV1 antagonist 3 Chemical Structure

TRPV1 antagonist 3 Chemical Structure

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Description

TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant[1].

IC50 & Target

hTRPV1

2.66 nM (IC50)

TRPM8

7.45 μM (IC50)

In Vitro

TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels[1].
TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL) [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel[1].
TRPV1 antagonist 3 (0-100 mg/kg; i.g.) had no obvious thermal effect in rats[1].
TRPV1 antagonist 3 (10 mg/kg; i.v.) shows a good concentration in the brain at 0.5 h, with value of 2311 ng/g, and has good CNS penetration, with a brain/plasma ratio of 1.66[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: KM male mice (18-22 g), capsaicin, acetic acid, and thermal induced pain model[1]
Dosage: 3, 10, and 30 mg/kg. 20 μL of solution of capsaicin (16 mg/20 mL) was injected s.c. under the skin of the dorsal surface of the right hind paw, or injected with 0.6% acetic acid (0.1 mL/10 g/mouse i.p.).
Administration: Intraperitoneally administration; 30 min
Result: In capsaicin-induced nociception, licking time decreased significantly in a dose-dependent manner. In acid-induced nociception, no significant anti-nociceptive activities were found compared with the control (SB-705498 and BCTC) at all dosage. In thermal-induced nociception, the latency time of nociceptive responses was increased at the doses of 10 and 30 mg/kg.
Animal Model: Spragur-Dawley male rats (220-250 g)[1]
Dosage: 10 mg/kg or 20 mg/kg
Administration: Intravenous injection of 10 mg/kg or oral dose of 20 mg/kg (Pharmacokinetic Analysis)
Result: In vivo pharmacokinetic parameters of TRPV1 antagonist 3 in rats (n=3)[1]
Parameters IV PO
t1/2 (h) 0.106 ± 0.076
t1/2, ka (h) 0.462 ± 0.096
t1/2, k10 (h) 0.527 ± 0.106
ka (1/h) 1.65 ± 0.364
k10 (1/h) 12.076 ± 2.337 1.133 ± 0.358
V (L/kg) 0.003 ± 0.001 0.016 ± 0.006
CL (L/h/kg) 0.024 ± 0.013 0.022 ± 0.01
Tmax (h) 0.711 ± 0.144
Cmax (ng/mL) 311.377 ± 108.017
AUC 0-inf (ng/mL*h) 495.955 ± 214.634 598.873 ± 212.319
MRT (h)
Molecular Weight

391.53

Appearance

Solid

Formula

C23H25N3OS

SMILES

CC(C1=CC=CC(NC(N2CCC[[email protected]]2C3=NC=C(S3)C4=CC=CC=C4)=O)=C1)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
TRPV1 antagonist 3
Cat. No.:
HY-144372
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