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KPR-2579

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

貨品編碼	規格	純度	價格 (￥)	現價(￥)	庫存描述	數量	總計 (￥)
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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中文別名	KPR-2579;KPR 2579;
英文別名	(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號	1801742-41-5
Inchi	Not available
InchiKey	Not available
分子式 Formula	C23H20F2N2O2
分子量 Molecular Weight	394.41
溶解度Solubility
性狀	powder；固體粉末
儲藏條件 Storage conditions	Store at room temp

白僵菌素, 來源于白僵菌是三聚環二肽，由交替的甲基苯基丙酰基和羥基戊酰基殘基組成。

它具有霉菌毒素，抗生素殺蟲劑，凋亡抑制劑，真菌代謝產物，離子載體，抗真菌劑，P450抑制劑和抗腫瘤劑的作用。

產品說明	KPR-2579，新型TRPM8拮抗劑，抑制大鼠乙酸誘導的膀胱傳入性機能亢進
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.

警示圖
危險性
危險性警示	Notavailable
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2416吸入可能對身體有害
安全防護	P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續沖洗+P337如果眼睛刺激持續+P2396獲得醫療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

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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