SB705498
目录号 : GC14580
SB705498是一种口服生物可利用的、竞争性的辣椒素介导的 TRPV1 受体拮抗剂（人类、大鼠和豚鼠的pKis分别为7.6、7.5和7.3）。SB705498能够快速、可逆地抑制辣椒素、酸或热介导的人类TRPV1激活。
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.
SB705498是一种口服生物可利用的、竞争性的辣椒素介导的TRPV1受体拮抗剂（人类、大鼠和豚鼠的pKis分别为7.6、7.5和7.3）。SB705498能够快速、可逆地抑制辣椒素、酸或热介导的人类TRPV1激活[1]。
SB705498（0.3nM-1μM；preincubated for 30min）可有效抑制辣椒素诱导的1321N1细胞或HEK293细胞中TRPV1蛋白激活，表观pKi分别为7.5或7.6[1]。SB705498（50nM；30min）可阻断静磁场对癌细胞凋亡的增强作用[2]。
SB705498（10mg；injected into the ventricle；one time） 不影响水分摄入的积累，并可在常氧条件下降低 [Ca2+][3]。SB705498(3-30mg/kg；po；2h pre-treatment time) 在10和30mg/kg口服剂量下表现出优异的活性，可很好地逆转异常性疼痛。SB705498在10mg/kg口服剂量下还显示出对豚鼠弗氏完全佐剂模型中异常性疼痛的80%逆转[4]。
| 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 | |
| 化学名 | 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 | ||
| 分子式 | C17H16BrF3N4O | 分子量 | 429.23 |
| 溶解度 | ≥ 14.5mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet