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49

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1541	Drospirenone ZK 3059,屈螺酮,Dihydrospirorenone	Glucocorticoid Receptor; Estrogen/progestogen Receptor; Progesterone Receptor; Androgen Receptor; COX	Endocrinology/Hormones; Immunology/Inflammation; Neuroscience; Others
	Drospirenone (ZK 3059) 是spironolactone 的类似物，是一种合成的孕酮。
T14856	Calcipotriol MC 903,卡泊三醇,Calcipotriene
	Calcipotriol (MC 903) 是一种合成的 VitD3类似物，对维他命 D 受体具有高亲和力。
T15196	EC23 BASF-46928,AGN 190205	Others	Others
	EC23 (AGN 190205) 是一种稳定的合成类视黄醇类似物，能够促使神经元分化。
TP1324	Melanotan (MT)-II 美拉诺坦 II,美拉诺坦 (MT)-II	Melanocortin Receptor	GPCR/G Protein; Neuroscience
	Melanotan (MT)-II 是一种可注射用的多肽荷尔蒙，是合成的黑皮质素受体激动剂，能够促进晒黑。
T12187L	Naspm trihydrochloride 1-Naphthylacetyl spermine trihydrochloride	iGluR	Membrane transporter/Ion channel; Neuroscience
	Naspm trihydrochloride (1-Naphthylacetyl spermine trihydrochloride) 是Joro 蜘蛛毒素的合成类似物，具有拮抗CP-AMPA 受体的活性。
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。
T1825	Reversine	Aurora Kinase; Adenosine Receptor; Autophagy	Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; GPCR/G Protein; Neuroscience
	Reversine 是一种 ATP-竞争性 Aurora kinase 抑制剂，作用于Aurora A、Aurora B 和Aurora C，IC50分别为 400、500 和 400 nM。
TP1434L	Lecirelin acetate(61012-19-9 free base)	GNRH Receptor	GPCR/G Protein
	Lecirelin acetate(61012-19-9 free base) 是一种合成的 GnRH（促性腺激素释放激素）类似物，在治疗牛卵巢滤泡囊肿方面显示出很好的疗效。
T7589	Afamelanotide acetate afamelanotide	Melanocortin Receptor	GPCR/G Protein; Neuroscience
	Afamelanotide acetate 是一种合成的 α-黑素细胞刺激激素类似物和一流的黑皮质素-1 受体激动剂，用于治疗红细胞生成性原卟啉症。
T0412	Idebenone 艾地苯醌,CV-2619	Apoptosis; Antioxidant; Mitochondrial Metabolism	Apoptosis; Metabolism; oxidation-reduction
	Idebenone (CV-2619) 是一种线粒体保护剂，具有神经保护功效，可用于研究阿尔茨海默病、亨廷顿舞蹈病，可透过血脑屏障，诱导细胞凋亡。
T40686	Tiazofurin NSC 286193,Riboxamide,噻唑呋林	Dehydrogenase	Metabolism
	Tiazofurin (NSC-286193) 是一种合成的核苷类似物，显示出抗肿瘤活性。它在细胞内合成为 tiazole-4-carboxamide adenine dinucleotide (TAD)，TAD 可有效抑制 IMP 脱氢酶。
TNU0130	2'-O-Methyl-2-thiouridine	Nucleoside Antimetabolite/Analog	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	2'-O-Methyl-2-thiouridine 是一种存在于合成嗜热细菌tRNA中的嘌呤核苷类似物。2'-O-Methyl-2-thiouridine 对 A 的选择性高于未修饰的 U。
TP2328L	CJC-1295 acetate(863288-34-0 free base) DAC:GRF acetate	GHSR	GPCR/G Protein
	CJC-1295 acetate(863288-34-0 free base) (DAC:GRF acetate) 是生长激素释放激素 (GHRH)（也称为生长激素释放因子 (GRF)）和生长激素促分泌素 (GHS) 的合成类似物。
T15095	Dehydroemetine	Others; Parasite	Microbiology/Virology; Others
	Dehydroemetine 是一种有效的抗原虫剂，是二盐酸艾美汀的合成类似物，可用于预防和治疗阿米巴感染和疾病，具有治疗伴有皮肤损伤的利什曼原虫感染和耐甲硝唑阿米巴病的作用。
T12908	SIBA 5'-Deoxy-5'-isobutylthioadenosine,5'-Isobutylthioadenosine,5ˊ-异丁硫基-5ˊ-脱氧腺苷	Nucleoside Antimetabolite/Analog; HSV	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	SIBA (5'-Deoxy-5'-isobutylthioadenosine) 是 SAH 的合成类似物，可作为 S-腺苷甲硫氨酸介导的甲基转移的抑制剂。它干扰多种酶活性，可逆地阻断单纯疱疹病毒 1 型病毒的繁殖。
T5019	Desmopressin 去氨加压素,DDAVP,Desmopressin Acetate	Vasopressin Receptor	GPCR/G Protein
	Desmopressin (DDAVP) 是抗利尿激素精氨酸加压素的合成类似物。
T6070	(E/Z)-Rigosertib sodium N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium	PLK	Cell Cycle/Checkpoint
	ON-01910 是一种非 ATP 竞争性 PLK1 抑制剂（IC50 为 9 nM，在无细胞试验中）。它对 Plk2 的选择性高出 30 倍，对 Plk3 没有活性。 Rigosertib 抑制 PI3K/Akt 通路并激活氧化应激信号。 Rigosertib 可诱导多种癌细胞凋亡。它是一种合成的苄基苯乙烯基砜类似物，具有潜在的抗肿瘤活性。
T6446	Clevudine L-FMAU,克拉夫定,Levovir	HBV; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	Clevudine (Levovir) 是一种非自然 L-构型的核苷类似物，是一种与聚合酶结合的非竞争性抑制剂，具有较强的抗 HBV 活性，半衰期长，毒性低的特点。
T20592	Cloprostenol Estrofan,Oestrophan
	Cloprostenol is a synthetic analogue of prostaglandin.
T12187	Naspm 1-Naphthylacetyl spermine	Others	Others
	Naspm is a synthetic analogue of Joro spider toxin and is a antagonist iscalcium permeable AMPA (CP-AMPA) receptors.
T13073	Taltobulin trifluoroacetate HTI-286 trifluoroacetate,SPA-110 trifluoroacetate	Others	Others
	Taltobulin trifluoroacetate is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.
T34056	PhTX-343 TFA (S)-PhTX 343,PhTX-343,(S)-PTX 343,(S)-Philanthotoxin 343,PhTX= 343
	PhTX-343, also known as Philanthotoxin 343, is synthetic analogue of Philanthotoxin 433. PhTX-343 blocks NMDA-gated ion channels; synthetic analog of the wasp polyamine amide toxin δ-philanthotoxin.
TP1172	Apraglutide FE 203799
	Apraglutide (FE 203799 is a synthetic 33-amino acid peptide and long-acting glp-2 analogue.
T31768	Fenestrel ORF 3858,AI3-62334
	Fenestrel is a synthetic, nonsteroidal estrogen that was developed as a postcoital contraceptive in the 1960s. Fenestrel is a seco analogue of doisynolic acid and a member of the cyclohexenecarboxylic acid series of estrogens.
T69669	Camsirubicin HCl
	Camsirubicin, also known as GPX-150, MNPR-201, and CNDO1011, is a synthetic non-cardiotoxic analogue of the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Anthracycline analogue GPX-150 intercalates DNA and impedes the activity of topoisomerase II, inducing single and double-stranded breaks in DNA; inhibiting DNA replication and/or repair, transcription, and protein synthesis; and activating tumor cell apoptosis.
T82917	BAY-R 1005
	BAY-R 1005为合成糖脂类似物(GLA)，具有免疫增强作用，能够调控抗体的合成。
T15560	Iloprost ZK 36374,Ciloprost,伊洛前列素	Others	Others
	Iloprost is a synthetic analogue of prostacyclin PGI2. Iloprost commonly employed in the treatment of peripheral vascular disease and also indicated in the treatment of patients affected by systemic sclerosis (SSc) in the presence of severe Raynaud's phen
TP1434	Lecirelin
	Lecirelin is a synthetic GnRH (gonadotropin releasing hormone) analogue which shows a great efficacy in the treatment of bovine ovarian follicular cysts.
T13073L	Taltobulin hydrochloride (228266-40-8 free base) SPA-110 hydrochloride,Taltobulin hydrochloride,HTI-286 hydrochloride	Others	Others
	Taltobulin hydrochloride is a synthetic analogue of the tripeptide hemiasterlin, is a potent agent of antimicrotubule that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.
T25374	Emofolin sodium NSC139490,MeTHHF disodium,NSC-139490,NSC 139490
	Emofolin sodium is the sodium salt of a synthetic antimetabolite analogue of folate with antineoplastic activity，which competes for the folate binding site of the enzyme dihydrofolate reductase, resulting in inhibition of tetrahydrofolate synthesis, deple
T16490	PF-06380101 Auristatin-0101,Aur0101	Others	Others
	PF-06380101 is an auristatin microtubule inhibitor and is a cytotoxic Dolastatin 10 analogue. When compared to other synthetic auristatin analogues that are used in the preparation of ADCs, PF-06380101 displays excellent potencies in tumor cell proliferat
T83546	(D-Trp8,D-Cys14)-Somatostatin-14
	"(D-Trp8,D-Cys14)-Somatostatin-14"为一种生长抑素合成类似物，主要用于代谢相关疾病研究。
T74349	AGD-0182
	AGD-0182为一种合成分子，是天然微管蛋白结合分子Dolastatin 10的类似物，具备微管破坏剂功能。
T83510	[Arg-15,20,21,Leu17]-PACAP-Gly-Lys-Arg-NH2 BM-PACAP
	[Arg-15,-20,-21,Leu17]-PACAP-Gly-Lys-Arg-NH2 (BM-PACAP) 为合成PACAP 1-27 类似物，展现出明显的松弛效应。
TP1171	Apraglutide TFA (1295353-98-8 free base) Apraglutide TFA,FE 203799e (TFA)
	Apraglutide TFA (FE 203799 TFA), a synthetic 33-amino-acid peptide and a long-acting GLP-2 analogue, enhances adaptation and linear intestinal growth in a neonatal piglet model of short bowel syndrome with total resection of the ileum.
T68326	Annamycin
	Annamycin is a semi-synthetic doxorubicin analogue annamycin with antineoplastic activity. Annamycin intercalates into DNA and inhibits topoisomerase II, resulting in the inhibition of DNA replication and repair and RNA and protein synthesis. This agent circumvents multidrug-resistance (MDR) transporters, including P-glycoprotein (P-gp).
T21886	HE-3235
	Apoptone 是 3β- 雄烷二醇合成类似物，是一种具有口服生物可利用度的抗癌剂。Apoptone 在前列腺癌和乳腺癌的啮齿类动物模型中具有活性。
T3694L	Tebanicline tosylate
	Tebanicline is a potent synthetic nicotinic (non-opioid) analgesic drug. It was developed as a less toxic analogue of the potent poison dart frog-derived compound epibatidine. Like epibatidine, tebanicline showed potent analgesic activity against neuropat
T27534	Herkinorin BF3DNCA methyl ester
	Herkinorin is an opioid analgesic and an analogue of the natural product Salvinorin A. herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A. Herkinorin is a semi-synthetic c
T76235	Peceleganan
	Peceleganan (PL-5) 是一种合成的肽类似物，由天蚕素 A (1-10) × 蜂毒素 B (3-18) 杂化而成，具有 (10+16) 的结构。该化合物具有抑制伤口感染的作用。
T76340	(Nle4)-α-MSH
	(Nle4)-α-MSH 是一种黑素细胞刺激激素α-MSH 的合成类似物。(Nle4)-α-MSH 能够使青蛙皮肤可逆变黑，并在热碱处理后表现出延长的活性。
T71768	CB10-277
	CB10-277 is a synthetic derivative of dimethylphenyl-triazene related to dacarbazine, with antineoplastic properties. Related to the agent dacarbazine, CB10-277 is converted in vivo to a monomethyl triazene form that alkylates DNA, resulting in inhibition of DNA replication and repair; in addition, this agent may act as a purine analogue, resulting in inhibition of DNA synthesis, and may interact with protein sulfhydryl groups.
T76001	Apraglutide TFA
	Apraglutide TFA (FE 203799 TFA) 是一种合成的、含33个氨基酸的肽类药物，为长效GLP-2类似物。它能在全回肠切除后导致的新生短肠综合征小猪中增强适应性和线性肠生长。
T41251	Taprostene
	Taprostene (CG-4203) 是一种合成的、化学稳定的前列环素 (PGI2) 类似物。Taprostene 对猫急性心肌缺血再灌注后内皮和心肌有保护作用。Taprostene 增强细胞保护作用，同时减少不必要的血液动力学影响。
T76235L	Peceleganan acetate
	Peceleganan (PL-5) acetate，一种人工合成的肽类似物，由天蚕素 A (1-10) 和蜂毒素 B (3-18) 杂化而成，具有 (10+16) 的结构。该化合物有效抑制伤口感染。
T37264	15(R)-15-methyl Prostaglandin D2 15(R)15methyl PGD2	GPR	Endocrinology/Hormones; GPCR/G Protein
	15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) 是一种 PGD2 合成类似物，也是一种具有选择性和强效性的 CRTH2/DP2 受体激动剂，可调节嗜酸性粒细胞 CD11b 表达、肌动蛋白聚合和趋化。
T75240	Taltobulin hydrochloride
	Taltobulin hydrochloride (HTI-286 hydrochloride) 是一种合成的三肽半胱氨酸类似物，为高效抗微管剂，能够在体内外绕过P-糖蛋白介导的药物耐药性。该化合物通过抑制微管蛋白的聚合和破坏细胞内微管结构，进而引起细胞有丝分裂停滞和细胞凋亡。
T71385	Aroplatin
	Aroplatin is a synthetic liposomal formulation of bis-neodecanoate diaminocyclohexane platinum (NDDP), a third-generation platinum complex analogue of cisplatin, with potential antineoplastic activity. After displacement of the 2 long-chain aliphatic leaving groups (neodecanoic acid), platinum diaminocyclohexane (DACH) complexes become highly reactive and alkylate macromolecules, forming both inter- and intra-strand DNA crosslinks and inhibiting DNA synthesis, which results in tumor cell cytotox...
T77995	NNZ 2591
	NNZ 2591为环状甘氨酸脯氨酸(cGP)小肽的合成类似物，具有口服活性，能穿过血脑屏障。在缺血性脑损伤模型中展现出神经保护作用，并改善帕金森病大鼠模型的运动功能，有望用于研究缺血性脑损伤和天使综合征。

化合物

Cat.No: T1541

Synonym: ZK 3059,屈螺酮,Dihydrospirorenone

Target: Glucocorticoid Receptor, Estrogen/progestogen Receptor, Progesterone Receptor, Androgen Receptor, COX

Cat.No: T14856

Synonym: MC 903,卡泊三醇,Calcipotriene

Cat.No: T15196

Synonym: BASF-46928,AGN 190205

Target: Others

Melanotan (MT)-II

Cat.No: TP1324

Synonym: 美拉诺坦 II,美拉诺坦 (MT)-II

Target: Melanocortin Receptor

Naspm trihydrochloride

Cat.No: T12187L

Synonym: 1-Naphthylacetyl spermine trihydrochloride

Target: iGluR

Cat.No: T22285

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

Target: Prostaglandin Receptor

Cat.No: T1825

Target: Aurora Kinase, Adenosine Receptor, Autophagy

Lecirelin acetate(61012-19-9 free base)

Cat.No: TP1434L

Target: GNRH Receptor

Afamelanotide acetate

Cat.No: T7589

Synonym: afamelanotide

Target: Melanocortin Receptor

Cat.No: T0412

Synonym: 艾地苯醌,CV-2619

Target: Apoptosis, Antioxidant, Mitochondrial Metabolism

Cat.No: T40686

Synonym: NSC 286193,Riboxamide,噻唑呋林

Target: Dehydrogenase

2'-O-Methyl-2-thiouridine

Cat.No: TNU0130

Target: Nucleoside Antimetabolite/Analog

CJC-1295 acetate(863288-34-0 free base)

Cat.No: TP2328L

Synonym: DAC:GRF acetate

Target: GHSR

Cat.No: T15095

Target: Others, Parasite

Cat.No: T12908

Synonym: 5'-Deoxy-5'-isobutylthioadenosine,5'-Isobutylthioadenosine,5ˊ-异丁硫基-5ˊ-脱氧腺苷

Target: Nucleoside Antimetabolite/Analog, HSV

Cat.No: T5019

Synonym: 去氨加压素,DDAVP,Desmopressin Acetate

Target: Vasopressin Receptor

(E/Z)-Rigosertib sodium

Cat.No: T6070

Synonym: N-[2-甲氧基-5-[[[2-(2,4,6-三甲氧基苯基)乙烯基]磺酰]甲基]苯基]甘氨酸钠盐,(E/Z) ON-01910 sodium

Target: PLK

Cat.No: T6446

Synonym: L-FMAU,克拉夫定,Levovir

Target: HBV, DNA/RNA Synthesis

Cat.No: T20592

Synonym: Estrofan,Oestrophan

Cat.No: T12187

Synonym: 1-Naphthylacetyl spermine

Target: Others

Taltobulin trifluoroacetate

Cat.No: T13073

Synonym: HTI-286 trifluoroacetate,SPA-110 trifluoroacetate

Target: Others

Cat.No: T34056

Synonym: (S)-PhTX 343,PhTX-343,(S)-PTX 343,(S)-Philanthotoxin 343,PhTX= 343

Cat.No: TP1172

Synonym: FE 203799

Cat.No: T31768

Synonym: ORF 3858,AI3-62334

Camsirubicin HCl

Cat.No: T69669

Cat.No: T82917

Cat.No: T15560

Synonym: ZK 36374,Ciloprost,伊洛前列素

Target: Others

Cat.No: TP1434

Taltobulin hydrochloride (228266-40-8 free base)

Cat.No: T13073L

Synonym: SPA-110 hydrochloride,Taltobulin hydrochloride,HTI-286 hydrochloride

Target: Others

Emofolin sodium

Cat.No: T25374

Synonym: NSC139490,MeTHHF disodium,NSC-139490,NSC 139490

Cat.No: T16490

Synonym: Auristatin-0101,Aur0101

Target: Others

(D-Trp8,D-Cys14)-Somatostatin-14

Cat.No: T83546

Cat.No: T74349

[Arg-15,20,21,Leu17]-PACAP-Gly-Lys-Arg-NH2

Cat.No: T83510

Synonym: BM-PACAP

Apraglutide TFA (1295353-98-8 free base)

Cat.No: TP1171

Synonym: Apraglutide TFA,FE 203799e (TFA)

Cat.No: T68326

Cat.No: T21886

Tebanicline tosylate

Cat.No: T3694L

Cat.No: T27534

Synonym: BF3DNCA methyl ester

Cat.No: T76235

Cat.No: T76340

Cat.No: T71768

Apraglutide TFA

Cat.No: T76001

Cat.No: T41251

Peceleganan acetate

Cat.No: T76235L

15(R)-15-methyl Prostaglandin D2

Cat.No: T37264

Synonym: 15(R)15methyl PGD2

Target: GPR

Taltobulin hydrochloride

Cat.No: T75240

Cat.No: T71385

Cat.No: T77995

Cat. No.	Product Name	Target	Signaling Pathways
T7992	4-Hydroxyflavanone	NO Synthase	Immunology/Inflammation
	4-Hydroxyflavanone 是一种黄酮的合成类似物，是 SREBP 成熟和脂质合成的抑制剂。它具有研究肝脏脂肪变性及血脂异常的潜力。
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。

天然产物

4-Hydroxyflavanone

Cat.No: T7992

Target: NO Synthase

Carboprost tromethamine

Cat.No: T14865

Target: Prostaglandin Receptor

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