1801742-41-5|KPR-2579|KPR-2579|-范德生物科技公司

KPR-2579

NMR下载 COA and HPLC MSDS下载
names：
KPR-2579
CAS号：
1801742-41-5
MDL Number：
MF(分子式)： C23H20F2N2O2 MW(分子量)： 394.41
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

货品编码	规格	纯度	价格 (¥)	现价(¥)	库存描述	数量	总计 (¥)
HCQ000121-1g	1g	97%	¥ 0.00	¥ 0.00	Get quote	- +	¥ 0.00
HCQ000121-25mg	25mg	97%	¥ 8350.00	¥ 8350.00	3-5weeks	- +	¥ 0.00
HCQ000121-5mg	5mg	97%	¥ 2780.00	¥ 2780.00	3-5weeks	- +	¥ 0.00

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中文别名	KPR-2579;KPR 2579;
英文别名	(αR)-α-[Benzoyl[(1R)-1-(3,5-difluorophenyl)ethyl]amino]-benzeneacetamide, N-((R)-2-Amino-2-oxo-1-phenylethyl)-N-((R)-1-(3,5-difluorophenyl)ethyl)benzamide, N-((R)-Carbamoylphenylmethyl)-N-[(R)-1-(3,5-difluorophenyl)ethyl]benzamide
CAS号	1801742-41-5
SMILES	O=C(C1=CC=CC=C1)N([C@H](C)C2=CC(F)=CC(F)=C2)[C@H](C3=CC=CC=C3)C(N)=O
Inchi	Not available
InchiKey	Not available
分子式 Formula	C23H20F2N2O2
分子量 Molecular Weight	394.41
闪点 FP	Not available
熔点 Melting point	Not available
沸点 Boiling point	Not available
Polarizability极化度
密度 Density	Not available
蒸汽压 Vapor Pressure
溶解度Solubility
性状	powder；固体粉末
储藏条件 Storage conditions	Store at room temp

白僵菌素, 来源于白僵菌是三聚环二肽，由交替的甲基苯基丙酰基和羟基戊酰基残基组成。

它具有霉菌毒素，抗生素杀虫剂，凋亡抑制剂，真菌代谢产物，离子载体，抗真菌剂，P450抑制剂和抗肿瘤剂的作用。

产品说明	KPR-2579，新型TRPM8拮抗剂，抑制大鼠乙酸诱导的膀胱传入性机能亢进
Introduction	KPR-2579, a Novel TRPM8 Antagonist, Inhibits Acetic Acid-Induced Bladder Afferent Hyperactivity in Rats
Application1
Application2
Application3

Aims:

Transient receptor potential melastatin 8 (TRPM8) is proposed to be a promising therapeutic target for hypersensitive bladder disorders. We examined the effects of KPR‐2579, a novel selective TRPM8 antagonist, on body temperature and on mechanosensitive bladder single‐unit afferent activities (SAAs) provoked by intravesical acetic acid (AA) instillation in rats.

Methods:
Female Sprague‐Dawley rats were used. Effects of cumulative intravenous (i.v.) administrations of KPR‐2579 (0.03‐1 mg/kg) on deep body temperature were investigated (N = 18). In separate animals, effects of bolus administration of KPR‐2579 (0.03 or 0.3 mg/kg, i.v.) on bladder hyperactivity induced by intravesical instillation of 0.1% AA were investigated using cystometry (N = 57) in a conscious free‐moving condition or urethane‐anesthetized condition, and SAA measurements (N = 41) were performed in a urethane‐anesthetized condition.

Results
KPR‐2579 at any doses tested did not affect body temperature. In cystometry measurements, a high dose (0.3 mg/kg) of KPR‐2579 counteracted the shortened intercontraction interval provoked by AA instillation. In SAA measurements, 48 single afferent fibers (n = 24 in each fiber) were isolated. AA instillations significantly increased the SAAs of C fibers, but not of Aδ fibers, in the presence of KPR‐2579's vehicle and a low dose (0.03 mg/kg) of KPR‐2579. Pretreatment with a high dose (0.3 mg/kg) of KPR‐2579 significantly inhibited the AA‐induced activation of C‐fiber SAAs.

警示图
危险性
危险性警示	Notavailable
安全声明	H303吞入可能有害+H313皮肤接触可能有害+H2416吸入可能对身体有害
安全防护	P264处理后彻底清洗+P280戴防护手套/穿防护服/戴防护眼罩/戴防护面具+P305如果进入眼睛+P351用水小心冲洗几分钟+P338取出隐形眼镜（如果有）并且易于操作,继续冲洗+P337如果眼睛刺激持续+P2396获得医疗建议/护理
备注	实验过程中防止吸入、食入，做好安全防护

Effects of TRPV4 cation channel activation on the primary bladder afferent activities of the rat. Aizawa N, Wyndaele JJ, Homma Y, Igawa Y. Neurourol Urodyn. 2012 Jan;31(1):148-55. doi: 10.1002

Avelino A, Cruz F. TRPV1 (vanilloid receptor) in the urinary tract: expression, function and clinical applications. Naunyn Schmiedebergs Arch Pharmacol 2006; 373: 287– 99

Yamada T, Ugawa S, Ueda T, Ishida Y, Kajita K, Shimada S. Differential localizations of the transient receptor potential channels TRPV4 and TRPV1 in the mouse urinary bladder. J Histochem Cytochem 200

Recent Progress in TRPM8 Modulation: An Update. González-Mu?iz R, Bonache MA, Martín-Escura C, Gómez-Monterrey I. Int J Mol Sci. 2019 May 28;20(11):2618. doi: 10.3390/ijms20112618. PMID: 31141957

Minagawa T, Aizawa N, Igawa Y, Wyndaele JJ. The role of transient receptor potential ankyrin 1 (TRPA1) channel in activation of single unit mechanosensitive bladder afferent activities in the rat. Neu

RQ-00434739, a novel TRPM8 antagonist, inhibits prostaglandin E2-induced hyperactivity of the primary bladder afferent nerves in rats.
Aizawa N, Ohshiro H, Watanabe S, Kume H, Homma Y, Igawa Y.Life Sci. 2019 Feb 1;218:89-95. doi: 10.1016/j.lfs.2018.12.031. Epub 2018 Dec 20.PMID: 30580018

The role of transient receptor potential ankyrin 1 (TRPA1) channel in activation of single unit mechanosensitive bladder afferent activities in the rat.
Minagawa T, Aizawa N, Igawa Y, Wyndaele JJ.Neurourol Urodyn. 2014 Jun;33(5):544-9. doi: 10.1002/nau.22449. Epub 2013 Jun 19.PMID: 23784920

KPR-5714, a Novel Transient Receptor Potential Melastatin 8 Antagonist, Improves Overactive Bladder via Inhibition of Bladder Afferent Hyperactivity in Rats.
Nakanishi O, Fujimori Y, Aizawa N, Hayashi T, Matsuzawa A, Kobayashi JI, Hirasawa H, Mutai Y, Tanada F, Igawa Y.J Pharmacol Exp Ther. 2020 May;373(2):239-247. doi: 10.1124/jpet.119.263616. Epub 2020 Feb 26.PMID: 32102918

KPR‐2579, a novel TRPM8 antagonist, inhibits acetic acid‐induced bladder afferent hyperactivity in rats.Naoki Aizawa,Yoshikazu Fujimori,Jun‐ichi,Kobayashi,Osamu,Nakanishi,Hideaki Hirasawa ,Haruki Kume,Yukio Homma,Yasuhiko Igawa;21 February 2018 https://doi.org/10.1002/nau.23532Citations: 6.

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