SB705498 |
| Catalog No.GC14580 |
SB705498 is an orally bioavailable, competitive antagonist of the capsaicin-mediated of TRPV1 receptors (pKis = 7.6; 7.5; and 7.3 for human, rat, and guinea pig, respectively).SB705498 rapidly and reversibly inhibits capsaicin-, acid-, or heat-mediated activation of human TRPV1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 501951-42-4
Sample solution is provided at 25 µL, 10mM.
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SB705498 is an orally bioavailable, competitive antagonist of the capsaicin-mediated of TRPV1 receptors (pKis = 7.6; 7.5; and 7.3 for human, rat, and guinea pig, respectively). SB705498 rapidly and reversibly inhibits capsaicin-, acid-, or heat-mediated activation of human TRPV1[1].
SB705498 (0.3nM-1μM; preincubated for 30min) potently inhibits capsaicin-induced activation of human TRPV1 expressed in 1321N1 cells or HEK293 cells with apparent pKi of 7.5 or 7.6, respectively[1]. SB705498 (50nM; 30min) blocked the enhanced effect of Static magnetic field on cancer cell apoptosis[2].
SB705498 (10mg; injected into the ventricle; one time) did not affect the accumulation of water intake and can reduce [Ca2+] under normoxia conditions[3]. SB705498 (3-30mg/kg; po; 2h pre-treatment time) displays excellent activity at 10 and 30mg/kg po with good reversal of allodynia. SB705498 is also shown to give 80% reversal of allodynia in the guinea pig Freund's Complete Adjuvant model at 10mg/kg p.o[4].
References:
[1]Gunthorpe M J, Hannan S L, Smart D, et al. Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 321(3): 1183-1192.
[2]Chen W T, Lin G B, Lin S H, et al. Static magnetic field enhances the anticancer efficacy of capsaicin on HepG2 cells via capsaicin receptor TRPV1[J]. PLoS One, 2018, 13(1): e0191078.
[3].Yang F, Zhou L, Wang D, et al. Suppression of TRPV4 channels ameliorates anti-dipsogenic effects under hypoxia in the subfornical organ of rats[J]. Scientific Reports, 2016, 6(1): 30168.
[4]Khan A, Khan S, Kim Y S. Insight into pain modulation: nociceptors sensitization and therapeutic targets[J]. Current drug targets, 2019, 20(7): 775-788.
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | The selective TRPV1 antagonist SB705498 was incubated with the cells 30min before Static magnetic field and capsaicin treatments. |
Reaction Conditions | SB705498 (50nM; 30min ) |
Applications | SB705498 blocked the enhanced effect of Static magnetic field on cancer cell apoptosis. |
| Animal experiment [2]: | |
Animal models | A model of anti-dipsia effect of the subfornical organ in rats under hypoxia |
Preparation Method | Thirst studies, all rats were deprived of water 1 day before the experiment and randomly divided into 8 groups: 1) normoxia + saline; 2) normoxia + 1μg gadolinium; 3) normoxia + 1μg HC-067047; 4) normoxia + 10 mg SB705498; 5) hypoxia + saline; 6) hypoxia + 1μg gadolinium; 7) hypoxia + 1μg HC-067047; 8) hypoxia + 10mg SB705498. Normoxic and hypoxic animals were placed in a sea level environment or a hypobaric chamber simulating an altitude of 6000 m for 6 h. 10 min before the experiment, 50μL of drug solution was injected into the cerebral ventricle using a microinjection cannula inserted into the guide cannula, and the control group without drug administration was continuously injected with an equal volume of sterile saline. Water consumption was measured 6h after hypoxia as (original water weight)-(current water weight). |
Dosage form | SB705498 (10mg; injected into the ventricle; one time) |
Applications | TRPV1 inhibitor, SB705498, did not affect the accumulation of water intake and can reduce [Ca2+] under normoxia conditions. |
References: | |
| Cas No. | 501951-42-4 | SDF | |
| Chemical Name | 1-(2-bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)pyridin-2-yl]pyrrolidin-3-yl]urea | ||
| Canonical SMILES | C1CN(CC1NC(=O)NC2=CC=CC=C2Br)C3=NC=C(C=C3)C(F)(F)F | ||
| Formula | C17H16BrF3N4O | M.Wt | 429.23 |
| Solubility | ≥ 14.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3298 mL | 11.6488 mL | 23.2975 mL |
| 5 mM | 0.466 mL | 2.3298 mL | 4.6595 mL |
| 10 mM | 0.233 mL | 1.1649 mL | 2.3298 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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