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20

抑制剂 & 化合物

5

天然产物

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Cat. No. Product Name Target Signaling Pathways
T10503 ACAT-IN-1 cis isomer

Acyltransferase Metabolism
ACAT-IN-1 cis isomer是一种有效的 ACAT 抑制剂(IC50:100 nM),可用于研究免疫系统相关疾病。
T6729 Lomibuvir

VX-222,VCH-222

HCV Protease Microbiology/Virology; Proteases/Proteasome
Lomibuvir (VCH-222) (VX-222) 是丙型肝炎病毒 NS5B 聚合酶的一种非核苷变构抑制剂,Kd 值为 17 nM,已证明具有临床疗效。Lomibuvir 抑制 1b/Con1 型 HCV 亚基因组复制子,EC50为 5.2 nM。Lomibuvir 优先抑制延长的 RNA 合成,而非从头合成的 RNA。
T1109 (Z)-Capsaicin

Zucapsaicin,Civamide,cis-Capsaicin,珠卡赛辛,(Z)-辣椒素

TRP/TRPV Channel; HSV Membrane transporter/Ion channel; Microbiology/Virology
(Z)-Capsaicin (Zucapsaicin) 是天然辣椒素的合成顺式异构体,用于治疗膝骨关节炎。它是一种可口服的 TRPV1激动剂,可研究神经性疼痛。
T13415 Zuclomiphene citrate

Others Others
Zuclomiphene citrate is a cis isomer of Clomiphene citrate, and has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer.
T74451 13-cis-Retinyl acetate

13-cis-Retinyl acetate (13-cis-Retinol acetate; 13-cis-Vitamin A acetate),视黄醇乙酸酯的13-顺式异构体,是维生素A的一个活性代谢物。
T71819 RK-20448

RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R, and Tie-2. It also inhibits BLK, Csk, Fyn, and Lyn. RK-20448 is the cis isomer of A-419259
T36236 5-cis Carbaprostacyclin

5-cis Carbaprostacyclin is a stable analog of PGI2 and an isomer of carbaprostacyclin. It is a weak inhibitor of human platelet aggregation with an IC50 of 2.8 μM compared to 0.3 μM for carbaprostacyclin. 5-cis Carbaprostacyclin is a much weaker effector of rabbit mesenteric artery relaxation with an EC50 of 104 μM compared to 5.9 μM for carbaprostacyclin. It even antagonizes the adenylate cyclase activation induced by carbaprostacyclin.
T37213 5-trans Latanoprost

Latanoprost is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. 5-trans Latanoprost is an isomer of latanoprost wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E). The trans isomer of latanoprost occurs as an impurity of between 2-5% in most commercial preparations of the bulk drug product. The present compound was prepared primarily as an analytical standard for detection and quantitation of this impurity. Fr...
T72436 cis,trans-Germacrone

cis,trans-Germacrone 是 Germacrone 的异构体。Germacrone 具有广泛的抗肿瘤、抗氧化和抗炎作用。Germacrone 抑制肺癌细胞增殖并改变 Akt/MDM2/p53。Germacrone 还能在 G1/S 期阻滞细胞周期。
T37214 5-trans Latanoprost (free acid)

Latanoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug. Latanoprost is an isopropyl ester, a prodrug form which is converted to latanoprost (free acid) by endogenous esterase enzymes. The free acid form is 200 times more potent than latanoprost as a ligand for the human recombinant FP receptor. 5-trans Latanoprost (free acid) is an isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from ci...
T73814 cis-Lomibuvir

cis-Lomibuvir (cis-VX-222) 是 Lomibuvir 的顺式异构体。Lomibuvir (VX-222) 是一种选择性的非核苷聚合酶抑制剂,靶向丙型肝炎病毒 NS5B 聚合酶 (RdRp) 的拇指口袋 2,Kd 为 17 nM。Lomibuvir 抑制 1b/Con1 型 HCV 亚基因组复制子,EC50为 5.2 nM。Lomibuvir 优先抑制延长的 RNA 合成,而非从头合成的 RNA。
T37230 (+)-5-trans Cloprostenol

Cloprostenol is a synthetic derivative of prostaglandin F2α that is used in veterinary medicine as a luteolytic agent for the induction of estrus and in the treatment of reproductive disorders in cattle, swine, and horses. (+)-5-trans Cloprostenol is a minor impurity produced in the synthesis of (+)-cloprostenol. The (+)-5-trans isomer is 20-fold less active than the 5-cis form in terminating pregnancy in the hamster.
T83878 Z-CITCO

Z-CITCO是构成型雄甾烷受体(CAR;在报告基因测定中,对人类受体的EC50 = 3.9 µM)的激动剂,同时也是CAR激动剂CITCO的顺式异构体。
T38220 11-cis Retinol

11-cisRetinol is an isomer of vitamin A . It is formed from vitamin A,viaatrans-retinyl ester intermediate, by the enzyme RPE65 in the retinal pigment epithelium and then converted to 11-cis retinal as part of the visual cycle.1,211-cisRetinol is an agonist of salamander and human red rod opsins expressed in COS cells and an inverse agonist of salamander red cone opsin, as well as human red and green cone opsins expressed in COS cells.3It promotes pigment formation in cone, but not rod, photorec...
T37547 trans-Urocanic Acid

trans-Urocanic acid is a major epidermal chromophore for the immunosuppressive effects of UV radiation that is produced in mammalian stratum corneum by the action of histidine ammonialyase on L-histidine. It contributes to the acidification of the surface of the stratum corneum, and its function has been proposed as that of an endogenous sunscreen, endowing a low-level of protection (SPF ~ 1.5) against UV-induced DNA damage and excessive keratinocyte apoptosis. Upon UVB exposure, trans-urocanic ...
T37396 13-epi-12-oxo Phytodienoic Acid

13-epi-12-oxo Phytodienoic acid (13-epi-12-oxo PDA) is a lipoxygenase metabolite of α-linolenic acid in the leaves of green plants such as corn. ω-3 and ω-6 polyunsaturated fatty acids in plants are substrates for plant lipoxygenases. 12-oxo PDA is one of the best studied end metabolites of this enzymatic pathway. While the initial enzymatic product and major isomer of 12-oxo PDA contains side chains in the cis position, both being β to the ring, the upper side chain attached at C-13, can and fr...
T69682 AEW541 HCl

AEW541, also known as NVP-AEW541, is a novel, potent IGF-IR kinase inhibitor. NVP-AEW541 is capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. Note: AEW541 has a Cis-configuration on the cyclobutane ring. Its CAS# is 475489-16-8. Many vendors and Sc-finder sc...
T35817 Photoswitchable PAD Inhibitor (technical grade)

Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK29...
T37305 6(S)-Lipoxin A4

6(S)-Lipoxin A4

The lipoxins are trihydroxy fatty acids containing a 7,9,11,13-conjugated tetraene. Lipoxin A4 (LXA4) was first described as a metabolite of 15-HpETE and/or 15-HETE when added in vitro to isolated human leukocytes. The material obtained in this manner consists of at least four distinct isomers: 5(S), 6(S); 5(S), 6(R); and the 11-trans and 11-cis isomers of each of these. 6(S)-LXA4 is one of the original four metabolites first identified by Serhan, Nicolaou, and Samuelsson. It was considered to b...
T35854 9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)

9(Z),11(E)-Conjugated linoleic acid is an isomer of linoleic acid that has been found in beef and milk fat.1It binds to peroxisome proliferator-activated receptor α (PPARα; IC50= 140 nM) and activates the receptor in a reporter assay using COS-1 cells expressing mouse PPARα when used at a concentration of 100 μM.29(Z),11(E)-Conjugated linoleic acid inhibits TNF-α-inducedGLUT4expression and increases insulin-stimulated glucose transport in 3T3-L1 adipocytes.3Dietary administration of 9(Z)11(E)-co...

化合物

ACAT-IN-1 cis isomer
Cat.No: T10503
Synonym:
Target: Acyltransferase
Lomibuvir
Cat.No: T6729
Synonym: VX-222,VCH-222
Target: HCV Protease
(Z)-Capsaicin
Cat.No: T1109
Synonym: Zucapsaicin,Civamide,cis-Capsaicin,珠卡赛辛,(Z)-辣椒素
Target: TRP/TRPV Channel, HSV
Zuclomiphene citrate
Cat.No: T13415
Synonym:
Target: Others
13-cis-Retinyl acetate
Cat.No: T74451
Synonym:
Target:
RK-20448
Cat.No: T71819
Synonym:
Target:
5-cis Carbaprostacyclin
Cat.No: T36236
Synonym:
Target:
5-trans Latanoprost
Cat.No: T37213
Synonym:
Target:
cis,trans-Germacrone
Cat.No: T72436
Synonym:
Target:
5-trans Latanoprost (free acid)
Cat.No: T37214
Synonym:
Target:
cis-Lomibuvir
Cat.No: T73814
Synonym:
Target:
(+)-5-trans Cloprostenol
Cat.No: T37230
Synonym:
Target:
Z-CITCO
Cat.No: T83878
Synonym:
Target:
11-cis Retinol
Cat.No: T38220
Synonym:
Target:
trans-Urocanic Acid
Cat.No: T37547
Synonym:
Target:
13-epi-12-oxo Phytodienoic Acid
Cat.No: T37396
Synonym:
Target:
AEW541 HCl
Cat.No: T69682
Synonym:
Target:
Photoswitchable PAD Inhibitor (technical grade)
Cat.No: T35817
Synonym:
Target:
6(S)-Lipoxin A4
Cat.No: T37305
Synonym: 6(S)-Lipoxin A4
Target:
9(Z),11(E)-Conjugated Linoleic Acid (sodium salt)
Cat.No: T35854
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T8137 (Z)-Aconitic acid

顺乌头酸,顺式乌头酸,Cls-Aconitic acid

Others; Endogenous Metabolite Metabolism; Others
(Z)-Aconitic acid 是 Aconitic acid 的顺式异构体。它是三羧酸循环中柠檬酸盐异构化为异柠檬酸盐的中间产物。
T37512 cis-4-Hydroxy-L-proline

Endogenous Metabolite Metabolism
cis-4-Hydroxy-L-proline 是脯氨酸的一种类似物,抑制胶原蛋白的产生。它通过阻止三层螺旋胶原在细胞层上的沉积从而抑制成纤维细胞的生长。它还可抑制原发性N-亚硝基甲基脲诱导的大鼠乳腺肿瘤的生长。
T40424 9-cis-Vitamin A palmitate

9-cis-Vitamin A palmitate,9-cis-Retinyl palmitate

9-cis-Vitamin A palmitate (9-cis-Retinyl palmitate) is a 9-cis isomer resulting from the interaction of vitamin A palmitate in corn flakes. It exhibits a biological activity of 26% compared to all-trans-vitamin A palmitate, which is known to be the most biologically active form of vitamin A.
T75679 13-cis-Vitamin A palmitate

13-cis-Vitamin A palmitate(13-cis-Retinyl palmitate)是一种在玉米片中发现的维生素A棕榈酸酯的13-顺式异构体。其生物活性相当于全反式维生素A棕榈酸酯(维生素A具生物活性形式)的75%。
T37911 cis-Resveratrol

顺式白藜芦醇,(Z)-Resveratrol

Resveratrol is a potent phenolic antioxidant found in grapes, red wine, and various berries that also has antiproliferative and anti-inflammatory activity. cis-Resveratrol is the double bond isomer of trans-resveratrol, the more often studied and naturally abundant of the two resveratrol isomers. cis-Resveratrol exhibits antioxidant activity in the &#181M range similar to that observed with trans-resveratrol. It blocks production of reactive oxygen species (ROS) by inhibition of NAD(P)H oxidase ...

天然产物

(Z)-Aconitic acid
Cat.No: T8137
Synonym: 顺乌头酸,顺式乌头酸,Cls-Aconitic acid
Target: Others, Endogenous Metabolite
cis-4-Hydroxy-L-proline
Cat.No: T37512
Synonym:
Target: Endogenous Metabolite
9-cis-Vitamin A palmitate
Cat.No: T40424
Synonym: 9-cis-Vitamin A palmitate,9-cis-Retinyl palmitate
Target:
13-cis-Vitamin A palmitate
Cat.No: T75679
Synonym:
Target:
cis-Resveratrol
Cat.No: T37911
Synonym: 顺式白藜芦醇,(Z)-Resveratrol
Target:
TargetMol Loading
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