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42

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T81576	PA22-2 IKVAV sequence,Laminin A-chain fragment
	PA22-2（IKVAV序列；层粘连蛋白A链片段）为一生物活性肽，源于小鼠层粘连蛋白a1氨基酸2110至2127残基。构成的细胞外基质能够促进神经突生长。
T81575	PA22-2 free acid Cys-Laminin A chain 2091-2108
	PA22-2 (free acid) (Cys-Laminin A chain 2091-2108) 为促进神经突生长和神经元样过程形成的多肽。该化合物适用于人腺样囊性癌细胞培养和肽功能化磷脂双层制备<sup>[3]。
T11875	LPA2 antagonist 2	LPA Receptor	GPCR/G Protein
	LPA2 antagonist 2 is ＞480-fold more selective than LPA3 (IC50 of 13.85 μM).LPA2 antagonist 2 is a selective LPA2 antagonist with an IC50 of 28.3 nM and a Ki of 21.1 nM.
T15786	LPA2 antagonist 1	Hydroxylase	Metabolism
	LPA2 antagonist 1 is an LPA2 antagonist (IC50: 17 nM).
T73237	gTPA2-OMe
	gTPA2-OMe 是潜在的钙钛矿型太阳能电池（PSC）空穴传输层候选材料。
T16798	RS 17053 hydrochloride RS-17053	Others; Adrenergic Receptor	GPCR/G Protein; Neuroscience; Others
	RS 17053 hydrochloride 是有效的、选择性的 α1A 肾上腺素受体 (α1A adrenoceptor) 拮抗剂。RS 17053 hydrochloride 在细胞膜中测得的 pKi 值为 9.1，功能分析的 pA2 值为 9.8。
TP1933	R715 TFA(185052-09-9 free base) R 715	Bradykinin Receptor	GPCR/G Protein
	R715 TFA(185052-09-9 free base) 是强效和选择性缓激肽 B1 受体拮抗剂 (pA2 = 8.49)。它对B2 受体无活性。它减少神经性疼痛小鼠模型中的机械性过度伤害感受。它代谢稳定。
T15682	L-371,257	Oxytocin Receptor; Vasopressin Receptor	Endocrinology/Hormones; GPCR/G Protein
	L-371,257 是催产素受体的竞争性拮抗剂，pA2 为 8.4，Ki 为 19 nM。 L-371,257 对加压素受体 1a 的 Ki 值为 3.7 nM。
T7817	Aprocitentan ACT-132577,N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]氨基磺酰胺	Endothelin Receptor	GPCR/G Protein
	Aprocitentan (ACT-132577) 是一种 Macitentan 的主要活性代谢物。它是 ETA/ETB 的双重拮抗剂，其 pA2值分别为 6.7 和 5.5，IC50分别为 3.4 nM 和 987 nM。
T10249	Adoprazine SLV313	Others	Others
	Adoprazine (SLV313) 是 5-HT 1A 受体的完全激动剂，其在 h5-HT1A 受体的 pEC50 为 9。Adoprazine 是 D2 和 D3 受体的完全拮抗剂，在 hD2 受体中的 pA2 值是 9.3，在 hD3 受体中的 pA2 值是 8.9。Adoprazine 具有非典型抗精神病的特征。
T11723L	JNJ-39758979	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	JNJ-39758979是一种选择性的、高亲和力的、可口服的组胺 H4 受体拮抗剂，具有抗炎和止痒作用，对人、小鼠和猴子的组胺 H4 受体的 Ki 值分别为 12.5、5.3 和 25 nM。它对组胺诱导的 cAMP 抑制作用具有拮抗作用，pA2 为 7.9。
T22921	LE 300	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	LE 300 是选择性多巴胺 D1 样受体拮抗剂，作用于人多巴胺 D1 和 D5 受体的Kis 分别为 1.9 nM 和 7.5 nM。在大鼠尾动脉实验中，它作用于5-HT2A 受体的pA2 为 8.32。
T8004	SNAP 94847 hydrochloride	GPR; Melanin-concentrating Hormone Receptor (MCHR)	Endocrinology/Hormones; GPCR/G Protein
	SNAP 94847 hydrochloride 是一种选择性黑色素浓缩激素受体1 拮抗剂，Ki 为 2.2 nM，具有抗抑郁样活性。它是 MCH 诱发的肌醇磷酸形成的高亲和力拮抗剂，pA2为 7.81。
T6364	Desfesoterodine 5-HMT,(R)-5-Hydroxymethyl Tolterodine,(R)-5-羟甲基托特罗定,PNU-200577,5-HM,5-hydroxymethyl Tolterodine	AChR	Neuroscience
	Desfesoterodine (5-HMT) 是选择性毒蕈碱受体拮抗剂，Kb 和pA2分别为 0.84 nM 和 9.14。它可改善大鼠脑梗死诱导膀胱过度活动，是 Tolterodine 和 Fesoterodine 的主要药理活性代谢产物。
T10516	Beperidium iodide SX 810	Others	Others
	Beperidium iodide is a competitive antagonist of the acetylcholine receptor (pA2: 7.93).
T13163	Tiotidine ICI 125211	Others	Others
	Tiotidine is a selective histamine H2-receptor antagonist (pA2=7.3-7.8 for guinea-pig right atrium).
T16034	Meclinertant SR 48692	Others	Others
	Meclinertant is an effective, selective, nonpeptide, and orally active neurotensin receptor 1 (NTS1) antagonist. Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization (pA2 : 8.13), in human colon carcinoma (HT-29) cell
T76427	(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B
	(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B 是 Neurokinin B(Neurokinin Receptor) 的竞争性拮抗剂，pA2 为 5.5，对 Substance P 或 Neurokinin A 没有影响。
T15647	Tipelukast MN 001,KCA 757	Leukotriene Receptor	GPCR/G Protein
	Tipelukast (KCA 757) 是一种新型可口服的白三烯受体 (leukotriene receptor) 拮抗剂，是具有抗炎活性，可减少纤维化，下调 TIMP-1、1 型胶原蛋白。Tipelukast 可用于研究哮喘疾病。
T27140	Delequamine HCl RS-15385,RS15385,RS 15385,Delequamine,RS-15385-197
	Delequamine HCl is a potent and selective alpha 2-adrenoceptor antagonist. Delequamine HCl has a pKi of 9.45 for alpha 2-adrenoceptors in the rat cortex (pA2 in the guinea-pig ileum of 9.72).
T36231	rac-7-hydroxy Propranolol (hydrochloride)
	rac-7-hydroxy Propranolol (hydrochloride) is a ring-hydroxylated isomer and metabolite of propranolol that is an antagonist at β-adrenergic receptors (0.95 potency relative to propranolol). It also demonstrates potent vasodilator activity (0.20 potency relative to propranolol; pA2 = 7.58).
T80137	(d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin d(CH2)5[Tyr(Me)2, Dab5]AVP	Vasopressin Receptor	GPCR/G Protein
	(d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin (d(CH2)5[Tyr(Me)2, Dab5]AVP)作为针对加压素受体V1a的特异性拮抗剂，具有pA2值为6.71。
T30880	Chir 2279 Chir2279
	Chir 2279 is a N-(substituted)glycine peptoid trimer with high-affinity binding for alpha 1-adrenoceptors. CHIR 2279 antagonized the epinephrine-induced increase in intraurethal pressure (pseudo pA2, 6.86) in dogs.
T36638	[Des-His1,Glu9]-Glucagon amide TFA [Des-His1,Glu9]-Glucagon amide TFA
	[Des-His1,Glu9]-Glucagon amide TFA is a potent peptide antagonist targeting the glucagon receptor, featuring a pA2 value of 7.2. It holds potential utility in diabetes pathogenesis research[1].
T63415	RXR antagonist 1
	RXR antagonist 1 是类视黄醇 X 受体 (Retinoid X Receptor (RXR)) 调节剂，表现出较高的 RXR 拮抗作用 (pA2: 8.06)。RXR antagonist 1 能够用于研究 2 型糖尿病。
TP2022	GR231118 GR 231118
	Potent neuropeptide Y (NPY) Y1 receptor antagonist (pA2 = 10 and 10.5 at rY1 and hY1, receptors respectively). Also a potent and selective NPY Y4 receptor agonist (pEC50 values are 6.0, 8.6 and 6.1 for rY2, hY4 and rY5 receptors respectively). Suppresses
T64078	MRS2179 tetrasodium hydrate
	MRS2179 tetrasodium hydrate 是 P2Y1 受体的竞争性拮抗剂，能够作用于火鸡 P2Y1 受体 (Kb: 102 nM, pA2: 6.99)，对血小板聚集表现出抑制作用。MRS2179 tetrasodium hydrate 对 P2Y1 的选择性高于 P2X1 (IC50: 1.15 μM)、P2X3 (IC50: 12.9 μM)、P2X2、P2X4、P2Y2、P2Y4 和 P2Y6 受体。
TP2091	Antisauvagine-30
	Potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM for binding to mouse CRF2β and rat CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells
TP1988	[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2
	Potent agonist of the nociceptin (ORL1) receptor, demonstrated both in vitro and in vivo. Selective, competitive antagonism at the nociceptin receptor has also been reported (pA2 = 7.02 and 6.75 in the guinea pig ileum and mouse vas deferens respectively)
T75909	[Nphe1]Nociceptin(1-13)NH2 TFA
	[Nphe1]Nociceptin(1-13) NH2 TFA 是一种 Nociceptin/orphanin FQ (NC)内源性配体，是一种选择性和竞争性的 ociceptin receptor 拮抗剂，不具有激动剂活性。[Nphe1]nociceptin(1-13)NH2 选择性结合重组 nociceptin 受体(pKi=8.4)，拮抗 nociceptin 对 CHO 细胞中 cAMP 积累的抑制作用(pA2=6.0)。[Nphe1]Nociceptin(1-13)NH2 有可能作为一种止痛试剂。
T27164	DHP-218 PAK-9,PAK9,PAK 9,DHP218
	DHP-218 is a calcium channel antagonist. DHP-218 inhibits Calcium-induced contraction of the rat aorta in high K+ solution with the pA2 value of 9.11. The IC50 value for the inhibitory effects of DHP-218 in high K+-induced and phenylephrine-induced contra
T28099	MRS2179 MRS 2179,MRS-2179
	MRS2179 is a competitive P2Y1 receptor antagonist (Kb = 100 nM) with no appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 µM, or at P2Y12 and P2Y13. It inhibits ADP-induced platelet shape change and aggregation (pA2 = 6.55) in vitro a
TP2033	[Des-His1,Glu9]-Glucagon amide des-His1-[Glu9]-Glucagon (1-29) amide
	Glucagon receptor antagonist (pA2 = 7.2 for inhibition of glucagon-induced adenylyl cyclase activation in rat liver membranes); displays no agonist activity. Enhances glucose-stimulated pancreatic insulin release in vitro. Blocks added glucagon-induced hy
T28884	SUN-C5174 SUNC-5174
	SUN-C5174 is a sleective 5-HT2 antagonist (pA2=8.98+/-0.06). SUN C5174 showed a marked inhibitory effect on the platelet aggregation induced by serotonin in combination with collagen and adenosine diphosphate (ADP) in canine or human platelet-rich plasma
T27703	JZP-361 JZP361,JZP 361	Lipase	Metabolism
	JZP-361 是一种特异性 MAGL 抑制剂，对人重组 MAGL、人重组 FAAH 和人 hABHD6 的 IC50 分别为 46 nM、7.24 μM 和 1.79 μM。 JZP-361 具有抗组胺活性。 JZP-361可用于哮喘研究。
T83807	Rp-Adenosine-5'-O-(1-thiotriphosphate) sodium Rp-ATP-α-S
	Rp-Adenosine-5'-O-(1-thiotriphosphate)（Rp-ATP-α-S）是一种含硫核苷酸衍生物ATP-α-S的异构体，同时也是嘌呤P2Y1受体的激动剂。在表达人类P2Y1受体的HEK293细胞中，Rp-ATP-α-S能增加钙的动员（EC50 = 75 nM）。该化合物与洗涤的人类孤立血小板结合（Ki = 156 nM），抑制由ADP引发的人类富血小板血浆（PRP）的聚集（pA2 = 4.74），并且能够抑制前列腺素E1（PGE1）在人类孤立PRP中引发的cAMP产生（pA2 = 5.26）。同时，Rp-ATP-α-S还能引起用氨基甲酰胆碱预先缩紧的豚鼠结肠条带的松弛（EC50 = 56 nM）。此外，Rp-ATP-α-S已经被用于合成被细菌核糖开关识别的环状二核苷酸。
T70267	ADL 08-0011 HCl
	ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg/kg) reverse...
T83688	R 715 TFA [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
	R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩（pA2 = 8.49）。R 715（200、400及600 µg/kg）通过尾部闪烁测试减少了由链脲佐菌素（STZ）诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白（MOG）（35-55）（MOG35-55）抗原肽诱导的实验性自体免疫性脑炎（EAE）小鼠模型中，通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率，改善对称步态，并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715（0.01 nmol/动物，脑室内）能在自发性高血压大鼠中降低平均动脉血压并增加心率。
T36618	Rupatadine
	Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu...
T17064	Tezosentan RO 610612	Others	Others
	Tezosentan is an antagonist of the endothelin receptor (pA2s: 9.5, 7.7 for ETA and ETB receptors, respectively).
T10501	YM158 free base YM-57158	Others	Others
	YM158 free base is a potent and selective antagonist of TXA2 and LTD4 receptor (pA2s: about 8.81 and 8.87).
T10351	Aprocitentan D4 ACT-132577 D4	Others	Others
	Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA/ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).

化合物

Cat.No: T81576

Synonym: IKVAV sequence,Laminin A-chain fragment

PA22-2 free acid

Cat.No: T81575

Synonym: Cys-Laminin A chain 2091-2108

LPA2 antagonist 2

Cat.No: T11875

Target: LPA Receptor

LPA2 antagonist 1

Cat.No: T15786

Target: Hydroxylase

Cat.No: T73237

RS 17053 hydrochloride

Cat.No: T16798

Synonym: RS-17053

Target: Others, Adrenergic Receptor

R715 TFA(185052-09-9 free base)

Cat.No: TP1933

Synonym: R 715

Target: Bradykinin Receptor

Cat.No: T15682

Target: Oxytocin Receptor, Vasopressin Receptor

Cat.No: T7817

Synonym: ACT-132577,N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧基]乙氧基]-4-嘧啶基]氨基磺酰胺

Target: Endothelin Receptor

Cat.No: T10249

Synonym: SLV313

Target: Others

Cat.No: T11723L

Target: Histamine Receptor

Cat.No: T22921

Target: Dopamine Receptor, 5-HT Receptor

SNAP 94847 hydrochloride

Cat.No: T8004

Target: GPR, Melanin-concentrating Hormone Receptor (MCHR)

Desfesoterodine

Cat.No: T6364

Synonym: 5-HMT,(R)-5-Hydroxymethyl Tolterodine,(R)-5-羟甲基托特罗定,PNU-200577,5-HM,5-hydroxymethyl Tolterodine

Target: AChR

Beperidium iodide

Cat.No: T10516

Synonym: SX 810

Target: Others

Cat.No: T13163

Synonym: ICI 125211

Target: Others

Cat.No: T16034

Synonym: SR 48692

Target: Others

(D-Pro2,D-Trp6,8,Nle10)-Neurokinin B

Cat.No: T76427

Cat.No: T15647

Synonym: MN 001,KCA 757

Target: Leukotriene Receptor

Delequamine HCl

Cat.No: T27140

Synonym: RS-15385,RS15385,RS 15385,Delequamine,RS-15385-197

rac-7-hydroxy Propranolol (hydrochloride)

Cat.No: T36231

(d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin

Cat.No: T80137

Synonym: d(CH2)5[Tyr(Me)2, Dab5]AVP

Target: Vasopressin Receptor

Cat.No: T30880

Synonym: Chir2279

[Des-His1,Glu9]-Glucagon amide TFA

Cat.No: T36638

Synonym: [Des-His1,Glu9]-Glucagon amide TFA

RXR antagonist 1

Cat.No: T63415

Cat.No: TP2022

Synonym: GR 231118

MRS2179 tetrasodium hydrate

Cat.No: T64078

Antisauvagine-30

Cat.No: TP2091

[Phe1Ψ(CH2-NH)Gly2]Nociceptin(1-13)NH2

Cat.No: TP1988

[Nphe1]Nociceptin(1-13)NH2 TFA

Cat.No: T75909

Cat.No: T27164

Synonym: PAK-9,PAK9,PAK 9,DHP218

Cat.No: T28099

Synonym: MRS 2179,MRS-2179

[Des-His1,Glu9]-Glucagon amide

Cat.No: TP2033

Synonym: des-His1-[Glu9]-Glucagon (1-29) amide

Cat.No: T28884

Synonym: SUNC-5174

Cat.No: T27703

Synonym: JZP361,JZP 361

Target: Lipase

Rp-Adenosine-5'-O-(1-thiotriphosphate) sodium

Cat.No: T83807

Synonym: Rp-ATP-α-S

ADL 08-0011 HCl

Cat.No: T70267

Cat.No: T83688

Synonym: [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH

Cat.No: T36618

Cat.No: T17064

Synonym: RO 610612

Target: Others

YM158 free base

Cat.No: T10501

Synonym: YM-57158

Target: Others

Aprocitentan D4

Cat.No: T10351

Synonym: ACT-132577 D4

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
TN3368	Akuammigine	Opioid Receptor; Adrenergic Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Akuammigine has in vitro antimalarial activity. Akuammigine competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptors, yielding pA2 values of 4.68. Akuammidine also shows a preference for mu-opioid binding sites with Ki val
TN5061	Stephanine	Adrenergic Receptor; Antifection	GPCR/G Protein; Microbiology/Virology; Neuroscience
	l-Stephanine is a potent and highly selective alpha 1 adrenoceptor blocker, inhibits anococcygeus muscle contraction induced by phenylephrine with pA2 values of 6.76. Stephanine shows significant antiplasmodial activities with IC(50) ranged from 1.2 uM to 52.3 uM. Stephanine and crebanine have high inhibitory activity against gram-positive animal pathogenic bacteria, with MIC values of 0.078-0.312g/l, but low inhibitory activity against gram-negative animal pathogenic bacteria, they also inhibit...
T19882	Bryonolic acid UNII-J7YR6A878I,20-epi-Bryonolic acid	Apoptosis; Antioxidant; Calcium Channel	Apoptosis; Membrane transporter/Ion channel; Metabolism; oxidation-reduction
	Bryonolic acid (20-epi-Bryonolic acid) 是一种从 Sandoricum indicum 提取的三萜类化合物，具有免疫调节、抗炎，抗氧化和抗癌等活性，通过抑制Ca2+内流和调节Ca2+-CaMKII-CREB信号通路中的基因表达来避免PC12细胞免受NMDA诱导的细胞凋亡反应。

天然产物

Cat.No: TN3368

Target: Opioid Receptor, Adrenergic Receptor

Cat.No: TN5061

Target: Adrenergic Receptor, Antifection

Cat.No: T19882

Synonym: UNII-J7YR6A878I,20-epi-Bryonolic acid

Target: Apoptosis, Antioxidant, Calcium Channel

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