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19

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T21902 ML351

Lipoxygenase Metabolism
ML351 是一种高度特异的15-LOX-1抑制剂,其 IC50=200 nM。它对 T1D 非肥胖糖尿病小鼠模型的血糖异常和β细胞氧化应激有抑制作用。它对相关同工酶 (5-LOX、血小板 12-LOX、15-LOX-2、绵羊 COX-1 和人 COX-2) 表现出良好的选择性(>250倍)。
T4552 Fursultiamine

Diteftin,呋喃硫胺,Judolor,Alinamin F

Others Others
Fursultiamine (Alinamin F) 是维生素 B1衍生物,具有抗伤害和抗肿瘤作用。它可用于研究维生素 B1缺乏病、骨关节炎和癌症。
T15247 ESI-05

NSC 116966

cAMP GPCR/G Protein
ESI-05 (NSC-116966) 是特异性的 cAMP 直接激活交换蛋白 2 (EPAC2) 拮抗剂(IC50:0.4 µM),能够抑制 cAMP 诱导的 EPAC2 的活化,并 EAPC2 介导的 Rap1 的活化。
T11571 HLY78

4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) 是 Wnt/β-catenin 信号通路的激活剂,通过靶向通道中 Axin 的 DIX 域,增强 Axin-LRP6 交联,诱导 Wnt 信号转导。
T7601L Carbetocin acetate

醋酸卡贝缩宫素,Carbetocin acetate(37025-55-1 free base),卡贝缩宫素醋酸盐

Oxytocin Receptor Endocrinology/Hormones; GPCR/G Protein
Carbetocin acetate 是催产素类似物,是催产素受体激动剂,Ki 是 7.1 nM。它对催产素受体的嵌合 N 末端具有高亲和力,Ki 为 1.17 μM。它能透过血脑屏障,可以通过激活 CNS 中的催产素受体而具有类抗抑郁活性,具有用于产后出血的研究潜力。
T22285 Carboprost

15(S)-15-Methyl Prostaglandin F2α,15-Methyl-PGF2α,卡前列素

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
Carboprost (15(S)-15-Methyl Prostaglandin F2α) 是一种前列腺素 F2α 的代谢稳定的合成类似物。它能够刺激子宫收缩并引起流产,可用于子宫收缩乏力引起的产后出血,以及在妊娠中期终止妊娠。
T7601 Carbetocin

卡贝缩宫素,醋酸卡贝缩宫素

Oxytocin Receptor Endocrinology/Hormones; GPCR/G Protein
Carbetocin 是催产素类似物,是催产素受体激动剂,Ki 是 7.1 nM。它对催产素受体的嵌合 N 末端具有高亲和力,Ki 为 1.17 μM。它能透过血脑屏障,可以通过激活 CNS 中的催产素受体而具有类抗抑郁活性,具有用于产后出血的研究潜力。
T70470 CM-352

MMP Proteases/Proteasome
CM-352是一种金属蛋白酶抑制剂,可减少脑损伤并改善脑出血大鼠模型的功能恢复。
T8857 LJP-1586 HCl

LJP 1586,LJP-1586 hydrochloride,LJP-1586,LJP1586

Others Others
LJP-1586 HCl 是一种高选择性的血管粘附蛋白-1(VAP-1)抑制剂,通过减少脑出血(ICH)后粘附分子表达和免疫细胞浸润而显示出抗炎作用。
T11662L INT-777

S-EMCA

GPCR19 GPCR/G Protein
INT-777(S-EMCA)是有效的 TGR5 激动剂,EC50 为 0.82 μM。 INT-777(S-EMCA)在大鼠蛛网膜下腔出血后通过 TGR3/cAMP/PKA 信号通路抑制 NLRP5-ASC 炎症小体介导的神经炎症。
T50100 3-hydroxy-3-phenylpentanamide

Others Others
3-hydroxy-3-phenylpentanamide 是一种手性化合物,属于β-羟基酰胺类。在神经病学中,它已被证明对缺血性脑损伤和脑出血具有神经保护作用。在精神病学中,它被研究为焦虑、抑郁和成瘾的潜在治疗方法。在肿瘤学中,它已被证明通过诱导细胞凋亡和抑制肿瘤生长而具有抗肿瘤活性。
T3560 Desmethylanethol trithione

ADT-OH

VEGFR; Akt Angiogenesis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
Desmethylanethol trithione (ADT-OH) 是合成硫化氢的供体。它利用上调 FADD 诱导细胞凋亡,并对体内黑色素瘤的形成具有一定的抑制作用,可用于研究癌症疾病。
T61677 piCRAC-1

piCRAC-1 is a powerful inhibitor of the photoinducible Ca2+ release-activated Ca2+ (CRAC) channel. It effectively alleviates thrombocytopenia and hemorrhage [1].
T38058 Cimetidine sulfoxide

Cimetidine sulfoxide (Cimetidine sulphoxide) is a metabolite of Cimetidine, functioning as a histamine H2-receptor antagonist with potential applications in treating peptic ulcer disease and upper gastrointestinal hemorrhage[1].
T11152 Edaravone-d5

MCI-186 D5

Others Others
Edaravone, a novel and potent free radical scavenger, effectively prevents MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator. Its deuterium-labeled variant, Edaravone D5, retains the original compound's attributes while offering isotopic labeling benefits.
TP1953 PG-931

PG 931

Potent and selective melanocortin 4 (MC4) receptor agonist (IC50 values are 0.58 and 55 nM for human MC4 and MC3 receptors respectively). Produces a rapid and dose dependent restoration of cardiovascular and respiratory function in hemorrhage-shocked rats
T73989 Tirilazad

Tirilazad是一种21-氨基类固醇非糖皮质激素,具有抑制脂质过氧化的能力。它对于脑或脊髓中因创伤、中风、缺血再灌注损伤所致的损害有减轻作用。此外,Tirilazad还展现出针对新型肺炎病毒的抗病毒活性,并在缺血性中风中提供神经保护,适用于蛛网膜下腔出血研究场景。
T70186 Methazolamide-d6

Methazolamide-d6 is intended for use as an internal standard for the quantification of methazolamide by GC- or LC-MS. Methazolamide is a carbonic anhydrase inhibitor. It reduces intraocular pressure and cerebrospinal fluid flow in a rat model of glaucoma. Methazolamide reduces electroshock-induced seizures in rats with an ED50 value of 19.2 mg/kg. It also inhibits production of reactive oxygen species (ROS) in a primary cortical neuron (PCN) cellular model of subarachnoid hemorrhage (SAH) and re...
T83851 Tat-QFNP12 TFA

Tat-QFNP12 是一种含有转录激活因子 (Tat) 跨膜结构域和抑制N-Myc下游调节基因2 (NDRG2) 与蛋白磷酸酶Mg2+/Mn2+依赖性1A (PPM1A) 蛋白-蛋白相互作用的肽。在以20 mg/kg剂量给药的内脑血管穿刺诱导的小鼠蛛网膜下腔出血模型中,它能减少由基质金属蛋白酶-9 (MMP-9) 浓度增高引起的血脑屏障内皮紧密连接的损失,减轻脑水肿,并且提高自发活动及肢体运动的对称性。

化合物

ML351
Cat.No: T21902
Synonym:
Target: Lipoxygenase
Fursultiamine
Cat.No: T4552
Synonym: Diteftin,呋喃硫胺,Judolor,Alinamin F
Target: Others
ESI-05
Cat.No: T15247
Synonym: NSC 116966
Target: cAMP
HLY78
Cat.No: T11571
Synonym: 4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine
Target: Wnt/beta-catenin
Carbetocin acetate
Cat.No: T7601L
Synonym: 醋酸卡贝缩宫素,Carbetocin acetate(37025-55-1 free base),卡贝缩宫素醋酸盐
Target: Oxytocin Receptor
Carboprost
Cat.No: T22285
Synonym: 15(S)-15-Methyl Prostaglandin F2α,15-Methyl-PGF2α,卡前列素
Target: Prostaglandin Receptor
Carbetocin
Cat.No: T7601
Synonym: 卡贝缩宫素,醋酸卡贝缩宫素
Target: Oxytocin Receptor
CM-352
Cat.No: T70470
Synonym:
Target: MMP
LJP-1586 HCl
Cat.No: T8857
Synonym: LJP 1586,LJP-1586 hydrochloride,LJP-1586,LJP1586
Target: Others
INT-777
Cat.No: T11662L
Synonym: S-EMCA
Target: GPCR19
3-hydroxy-3-phenylpentanamide
Cat.No: T50100
Synonym:
Target: Others
Desmethylanethol trithione
Cat.No: T3560
Synonym: ADT-OH
Target: VEGFR, Akt
piCRAC-1
Cat.No: T61677
Synonym:
Target:
Cimetidine sulfoxide
Cat.No: T38058
Synonym:
Target:
Edaravone-d5
Cat.No: T11152
Synonym: MCI-186 D5
Target: Others
PG-931
Cat.No: TP1953
Synonym: PG 931
Target:
Tirilazad
Cat.No: T73989
Synonym:
Target:
Methazolamide-d6
Cat.No: T70186
Synonym:
Target:
Tat-QFNP12 TFA
Cat.No: T83851
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T14865 Carboprost tromethamine

Prostaglandin Receptor GPCR/G Protein; Immunology/Inflammation
Carboprost tromethamine 是合成的前列腺素 F2α的15-甲基类似物,能有效促进子宫的规律收缩,显着减少产中及产后出血量。
T66582 6-Methylnicotinamide

Endogenous Metabolite Metabolism
6-Methylnicotinamide 是烟酰胺的衍生物,是一种内源性代谢物。在脑出血 (ICH) 急性期, 6-Methylnicotinamide 突然增加会加剧神经损伤。6-Methylnicotinamide 可用于制作共晶体/盐。
T3976 Cytosporone B

Csn-B,Dothiorelone G

Others Others
Cytosporone B (Dothiorelone G) 是一种天然存在的核孤儿受体Nur77/NR4A1激动剂(EC50=0.278 nM)。
TN4937 Sambutoxin

Others Others
Sambutoxin, a new mycotoxin produced by toxic Fusarium isolates obtained from rotted potato tubers, it can cause toxic effects in rats, including body weight loss, feed refusal, hemorrhage in the stomach and intestines, and, finally, death when rats were

天然产物

Carboprost tromethamine
Cat.No: T14865
Synonym:
Target: Prostaglandin Receptor
6-Methylnicotinamide
Cat.No: T66582
Synonym:
Target: Endogenous Metabolite
Cytosporone B
Cat.No: T3976
Synonym: Csn-B,Dothiorelone G
Target: Others
Sambutoxin
Cat.No: TN4937
Synonym:
Target: Others
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