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

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.

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TRPV1 antagonist 3 Chemical Structure

TRPV1 antagonist 3 Chemical Structure

CAS No. : 2765294-54-8

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Based on 1 publication(s) in Google Scholar

TRPV1 antagonist 3 Related Antibodies

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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].

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

TRPV1 antagonist 3 Related Antibodies
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].

MedChemExpress (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
Molecular Weight

391.53

Formula

C23H25N3OS
CAS No.
Appearance

Solid

Color

Off-white to pale purple

SMILES

CC(C1=CC=CC(NC(N2CCC[C@H]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
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (255.41 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5541 mL 12.7704 mL 25.5408 mL
5 mM 0.5108 mL 2.5541 mL 5.1082 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5541 mL 12.7704 mL 25.5408 mL 63.8521 mL
5 mM 0.5108 mL 2.5541 mL 5.1082 mL 12.7704 mL
10 mM 0.2554 mL 1.2770 mL 2.5541 mL 6.3852 mL
15 mM 0.1703 mL 0.8514 mL 1.7027 mL 4.2568 mL
20 mM 0.1277 mL 0.6385 mL 1.2770 mL 3.1926 mL
25 mM 0.1022 mL 0.5108 mL 1.0216 mL 2.5541 mL
30 mM 0.0851 mL 0.4257 mL 0.8514 mL 2.1284 mL
40 mM 0.0639 mL 0.3193 mL 0.6385 mL 1.5963 mL
50 mM 0.0511 mL 0.2554 mL 0.5108 mL 1.2770 mL
60 mM 0.0426 mL 0.2128 mL 0.4257 mL 1.0642 mL
80 mM 0.0319 mL 0.1596 mL 0.3193 mL 0.7982 mL
100 mM 0.0255 mL 0.1277 mL 0.2554 mL 0.6385 mL
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TRPV1 antagonist 3 Related Classifications

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.

Keywords:

TRPV1 antagonist 32765294-54-8TRP ChannelTransient receptor potential channelsCNS penetrationKM male micecapsaicinTRPM8Inhibitorinhibitorinhibit

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