Cayman热销产品—Coenzyme A (lithium salt hydrate) (货号:21499)

Cayman热销产品—Coenzyme A (lithium salt hydrate) (货号:21499)

辅酶A (CoA)是一种重要的辅助因子,在柠檬酸循环和脂肪酸代谢中充当酰基载体和羰基活化基团。大约4%的细胞酶利用CoA作为底物。它是由泛酸通过需要ATP的5个步骤合成的。辅酶A生物合成途径中的泛酸激酶步骤已被确定为抗菌化合物开发的靶点。

产品结构:

 

产品详情:

货号:21499

产品名称:Coenzyme A (lithium salt hydrate) 

CAS号:85-61-0

分子式:C21H33N7O16P3S • 3Li [XH2O]

别名:CoA

分子量:785.3

纯度:≥95% (NMR)

形式:A crystalline solid

详情请咨询 Cayman 中国代理-上海金畔生物    

Benzamil Hydrochloride Hydrate

Benzamil Hydrochloride Hydrate

货号:
IB2910

品牌:
Jinpan

Benzamil Hydrochloride Hydrate

产品简介
浓度 ≥98%
有效期 2年
描述 Benzamil hydrochloride 是钠通道(ENaC)的特异性阻断剂。
MDL MFCD00069219
CAS 161804-20-2
分子式 C13H14ClN7O·HCl·xH2O
分子量 356.21 (Anhydrous)
储存条件 2-8℃
外观(性状) Solid
单位
SMILES O=C(C1=NC(Cl)=C(N)N=C1N)NC(NCC2=CC=CC=C2)=N.[H]Cl
靶点 Sodium Channel
规格 10mg

培美曲塞二钠水合物

培美曲塞二钠水合物

货号:
IP0130

品牌:
Jinpan

培美曲塞二钠水合物

暂无详情

培美曲塞二钠水合物

暂无详情
产品简介
别名 Pemetrexed (disodium hemipenta hydrate) (1:2:2.5) ;Pemetrexed sodium hydrate; Pemetrexed disodium hemipenta hydrate ; LY231514 disodium hemipenta hydrate
英文名称 Pemetrexed Disodium
CAS 357166-30-4
分子式 2(C20H19N5Na2O6)·5(H2O)
分子量 1032.84
纯度 HPLC≥98%
单位
生物活性 Pemetrexed disodium hemipenta hydrate 是一种叶酸拮抗剂 (antifolate)。抑制胸苷酸合成酶 (TS),二氢叶酸还原酶 (DHFR) 和甘氨酰胺核苷酸甲酰转移酶 (GARFT),Ki 分别为 1.3 nM,7.2 nM 和 65 nM。[1-2]
IC50 Ki: 1.3 nM (TS), 7.2 nM (DHFR), 65 nM (GARFT)[1]
In Vitro 培美曲塞(LY231514)二钠是一种新型经典抗叶酸剂,其抗肿瘤活性可能是由于其多聚谷氨酸化代谢物同时和多重抑制几种关键的叶酸需要酶。培美曲塞(LY231514)是已知用于FPGS的最佳底物之一(Km =1.6μM和Vmax/Km = 621)。多糖化和LY231514的多谷氨酸化代谢物可能在确定该新药的选择性和抗肿瘤活性方面发挥重要作用。尽管LY23154仅适度抑制TS(Ki = 340nM,重组小鼠),但LY23154的戊谷氨酸的效力是100倍(Ki = 3.4nM),使得LY231514成为最有效的基于叶酸的TS抑制剂之一[1]。
In Vivo 用PC61加培美曲塞治疗的小鼠组在统计学上显示出比其他组更长的存活期。在生存分析中,与单用PC61,大鼠IgG加培美曲塞治疗或未治疗的患者相比,用PC61加培美曲塞治疗的小鼠组观察到明显更好的生存[2]。
激酶实验 通过在A298监测由10-甲酰基 – [6R,S] -5,6,7,8-四氢叶酸的[6S] -5,6,7,8-四氢叶酸的形成,在室温下进行AICARFT抑制试验。所有溶液在使用前用N 2气体吹扫。反应溶液含有33mM Tris-Cl,pH 7.4,25mM KCl,5mM 2-巯基乙醇,0.05mM AICA核糖核苷酸和16nM(2毫单位/ mL)AICARFT。使用10-甲酰基 – [6R,S] -5,6,7,8-四氢叶酸盐浓度0.037,0.074和0.145mM(分别为其Km值的0.61,1.23和2.45倍)。测试LY231514作为0.08-0.8mM(四种浓度)的抑制剂。当LY231514的三 – 和五谷氨酸盐用作抑制剂时,浓度为0.0005-0.009mM(八种浓度)。通过添加酶引发酶测定。使用ENZFITTER程序分析数据以进行竞争性抑制。
SMILES O=C([O-])CC[C@@H](C([O-])=O)NC(C1=CC=C(CCC2=CNC(N=C(N)N3)=C2C3=O)C=C1)=O.[Na+].[2.5H2O].[Na+]
靶点 Antifolate
动物实验 产生剂量 – 反应曲线以确定50%生长抑制所需的浓度(IC 50)。培美曲塞最初以4mg/mL的浓度溶解于DMSO中,并进一步用细胞培养基稀释至所需浓度。将完全培养基中的CCRF-CEM白血病细胞加入到24孔Cluster平板中,终浓度为4.8×104细胞/孔,总体积为2mL。将各种浓度的测试化合物加入到两个孔中,使得DMSO的最终体积为0.5%。将板在37℃,5%CO 2的空气气氛中温育72小时。在孵育结束时,在ZBI Coulter计数器上测定细胞数。对照孔通常在孵育结束时含有4×105至6×10 5个细胞。对于一些研究,在300μMAICA,5μM胸苷,100μM次黄嘌呤或5μM嘧啶加100μM次黄嘌呤的组合存在下测定每种化合物的IC50 [1]。
细胞实验 产生剂量 – 反应曲线以确定50%生长抑制所需的浓度(IC 50)。培美曲塞最初以4mg/mL的浓度溶解于DMSO中,并进一步用细胞培养基稀释至所需浓度。将完全培养基中的CCRF-CEM白血病细胞加入到24孔Cluster平板中,终浓度为4.8×10 4细胞/孔,总体积为2mL。将各种浓度的测试化合物加入到两个孔中,使得DMSO的最终体积为0.5%。将板在37℃,5%CO 2的空气气氛中温育72小时。在孵育结束时,在ZBI Coulter计数器上测定细胞数。对照孔通常在孵育结束时含有4×105至6×10 5个细胞。对于一些研究,在300μMAICA,5μM胸苷,100μM次黄嘌呤或5μM嘧啶加100μM次黄嘌呤的组合存在下测定每种化合物的IC50 [1]。
数据来源文献 [1]. Shih C, et al. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23.

[2]. Anraku M, et al. Synergistic antitumor effects of regulatory T cell blockade combined with pemetrexed in murine malignantmesothelioma. J Immunol. 2010 Jul 15;185(2):956-66.

规格 10mg 10mM*1mL (in Water) 50mg

是一种叶酸拮抗剂。抑制胸苷酸合成酶 (TS),二氢叶酸还原酶 (DHFR) 和甘氨酰胺核苷酸甲酰转移酶 (GARFT)。

Alendronate sodium hydrate

Alendronate sodium hydrateCAS号: 121268-17-5分子式: C4H13NO7P2.3H2O.Na分子量: 325.13描述纯度储存/保存方法别名外观可溶性/溶解性In vitro(体外研究)In vivo(体内研究)

产品描述
描述

Alendronate (Fosamax) is a farnesyl diphosphate synthase inhibitor with IC50 of 460 nM. It is a nitrogen-containing bisphosphate that acts as a robust inhibitor of bone resorption and induces apoptosis in osteoclasts. It causes disruption of the ruffled border and actin cytoskeleton of osteoclasts and induces in vitro apoptosis of osteoclasts and macrophages by inhibiting farnesyl diphosphate synthase (IC50 = 460 nM). It efficiently chelates metal ions and functions as a broad-spectrum MMP inhibitor (IC50 ~ 40 – 70 uM). And it also displays antimetastatic, anti-invasive and cell-adhesion-promoting properties (IC50 ~ 1 pM, in vitro invasion of prostate cancer cells).

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
阿仑膦酸钠;Alendronate;MK 217;G-704650 Adronat
外观
white solid
可溶性/溶解性
DMSO :20 mg/mL (61.3 mM) with gentle warming
Water :20 mg/mL (61.3 mM) with gentle warming
生物活性
In vitro(体外研究)
Alendronate, acting directly on osteoclasts, inhibits a rate-limiting step in the cholesterol biosynthesis pathway, essential for osteoclast function. Alendronate inhibits the isoprenoid biosynthesis pathway and interferes with protein prenylation, as a result of reduced geranylgeranyl diphosphate levels. Alendronate inhibits the incorporation of mevalonolactone into proteins of 18-25 kDa and into nonsaponifiable lipids, including sterols in osteoclasts. Alendronate causes a dose-dependent inhibition of MVA incorporation into sterols and a concomitant increase in incorporation of radiolabel into IPP and DMAPP.
In vivo(体内研究)
Alendronate causes erosions in the rabbit stomach, but not antral ulceration in rats. Alendronate increases the incidence and size of indomethacin-induced antral ulcers. Alendronate also enhances indomethacin-induced gastricdamage in the rat, and delayed gastric ulcer healing. Alendronate (0.04-0.1 mg/kg twice weekly or 0.1 mg/kg weekly) partially blocks the establishment of bone metastases by human PC-3 ML cells and results in tumor formation in the peritoneum and other soft tissues. Alendronate pretreatment of mice (0.1 mg/kg twice weekly or weekly) and dosing along with taxol (10-50 mg/kg/day, twice weekly, or weekly) blocks the growth of PC-3 ML tumors in the bone marrow and soft tissues in a statistically significant manner and improves survival rates significantly by 4-5 weeks.

分子结构图

Alendronate sodium hydrate

Levofloxacin (hydrate) 左氧氟沙星

Levofloxacin (hydrate) 左氧氟沙星

货号:
IL0090

品牌:
Jinpan

Levofloxacin (hydrate)  左氧氟沙星

暂无详情
产品简介
EC EINECS 604-067-2
MDL MFCD07772024
别名 乳酸左氧氟沙星
CAS 138199-71-0
分子式 C18H20FN3O4·1/2H2O
分子量 370.38
纯度 HPLC≥98%
单位
SMILES O=C(C(C1=O)=CN2[C@@H](C)COC3=C(N4CCN(C)CC4)C(F)=CC1=C23)O.[0.5H2O]
靶点 Bacterial;Topoisomerase
规格 50mg 10mM*1mL in DMSO 100mg

是抗生素化合物,抑制细菌DNA旋转酶活性。

Morin hydrate;桑色素

Morin hydrate;桑色素

货号:
IM0620

品牌:
Jinpan

Morin hydrate;桑色素

暂无详情
产品简介
MDL MFCD00006826
EC EINECS 207-542-9
别名 桑黄素;AluminumIonophoreI
英文名称 Morin hydrate
CAS 480-16-0
分子式 C15H10O7
分子量 302.24
纯度 HPLC≥98%
单位
SMILES O=C1C(O)=C(C2=CC=C(O)C=C2O)OC3=CC(O)=CC(O)=C13
靶点 Others
规格 5mg 10mg 20mg
Morin 是一种植物性黄酮类化合物。

AH 23848, calcium salt hydrate

AH 23848, calcium salt hydrate分子式: [C29H34NO5]2•Ca2+分子量: 993.25描述应用储存/保存方法形态IC50可溶性/溶解性

产品描述
描述
Thromboxane (TXA2) activates the T prostanoid (TP) receptor. Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. AH-23848 is a dual antagonist of TP1 and EP4 receptors. It originally was found to inhibit TXA2-induced platelet aggregation (IC50 = 0.26 μM) and the contraction of human bronchial smooth muscle induced by the TP agonist U-46619. AH-23848 was subsequently demonstrated to impair PGE2-mediated relaxation of piglet saphenous vein by antagonizing the PGE2 receptor EP4. Through inhibiting EP4, it likewise suppresses serum-induced cAMP generation, cyclin A synthesis, as well as the proliferation of fibroblasts, as well as reduces metastasis in a murine model of metastatic breast cancer.
应用
An activator of T prostanoid receptor
储存/保存方法
Store at -20° C
形态
Solid
基本信息
IC50
TXA2-induced platelet aggregation: IC50 = 0.26 µM
可溶性/溶解性
Soluble in DMSO (~5 mg/ml).

CX-6258 hydrochloride hydrate

CX-6258 hydrochloride hydrateCAS号: 1353858-99-7分子式: C26H27Cl2N3O4分子量: 516.42描述纯度储存/保存方法别名可溶性/溶解性靶点

产品描述
描述

CX-6258 hydrochloride hydrate is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
CX6258 hydrochloride hydrate, CX 6258 hydrochloride hydrate
可溶性/溶解性
10 mM in DMSO
生物活性
靶点
Pim

分子结构图

CX-6258 hydrochloride hydrate