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Cat. No.	Product Name	Target	Signaling Pathways
T21874	CID 2745687	GPR	Endocrinology/Hormones; GPCR/G Protein
	CID 2745687 是可逆的、特异性 GPR35竞争性拮抗剂（Ki:12.8 nM）。
T8423	ML417	Dopamine Receptor; Arrestin	GPCR/G Protein; Neuroscience
	ML417 是选择性的，可透过血脑屏障的 D3 多巴胺受体激动剂，EC50=38 nM。它能够促进 D3R 介导的 β-arrestin 易位、G 蛋白介导的信号传导和 pERK 磷酸化，对其他 GPCR 介导的信号传导影响小。它对毒素诱导的多巴胺能神经元变性具有神经保护活性。
T26869	BMS-986122 BMS 986122	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	BMS-986122 (BMS 986122) 是选择性 μ 阿片受体正变构调节剂，可增加 β-抑制蛋白募集、腺苷酸环化酶抑制和 G 蛋白活化的作用，还增强 DAMGO 介导的 [35S]GTPγS 在小鼠脑膜中的结合。
T28073	MLS1547 MLS000051547,MLS 1547,MLS-1547	Dopamine Receptor	GPCR/G Protein; Neuroscience
	MLS1547 (MLS000051547) 是一种高效的 G 蛋白偏向多巴胺 D2 受体激动剂，Ki 为 1.2 μM。 MLS1547 在钙动员试验中刺激 D2R G 蛋白介导的信号传导，EC50 为 0.37 μM。
T12006	Metarrestin ML246	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	Metarrestin (ML246) 是一种口服有效的选择性核仁周区室 (PNC) 抑制剂，可有效抑制转移。Metarrestin 破坏核仁结构并抑制 RNA 聚合酶 (Pol) I 转录，部分是通过与翻译延伸因子 eEF1A2 的相互作用。
T15183	Dynarrestin	Hedgehog/Smoothened	GPCR/G Protein; Stem Cells
	Dynarrestin 是一种细胞质动力蛋白 1 和 2的氨基噻唑抑制剂。它能够快速的、可逆的抑制动力蛋白 1 驱动的微管在体外滑动和细胞内动力蛋白 1 和 2 依赖性过程，且不影响 ATP 水解和干扰纤毛发生。它可抑制神经元前体和肿瘤细胞的刺猬因子依赖性增殖。
T61562	CB1R Allosteric modulator 3	cAMP; Cannabinoid Receptor	GPCR/G Protein
	CB1R Allosteric modulator 3 是一种有效的 CB1R 调制剂。CB1R Allosteric modulator 3 抑制 cAMP 和 β-Arrestin ，可用于研究肥胖和尼古丁成瘾。
T23434	GPR35 agonist 2 TC-G 1001	GPR; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	GPR35 agonist 2 (TC-G 1001) 是一种有效的 GPR35 激动剂。GPR35 agonist 2 在 β-arrestin 和 Ca2+ 释放试验中的 EC50 值分别为 26 和 3.2 nM。
T33452	ML192 ML-192,CID1434953,CID 1434953,ML 192,CID-1434953	Cannabinoid Receptor; GPR; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	ML192 (CID1434953) 是一种具有选择性的 GPR55 配体拮抗剂。ML192 是一种抑制剂，可抑制 β-arrestin 转运、ERK1/2 磷酸化和 PKCβII 易位。
T4390	ML221	Apelin receptor; Arrestin	GPCR/G Protein
	ML221 是apelin (APJ)拮抗剂，能够抑制 apelin-13 介导的 APJ 的活化，在 cAMP 试验和 β-arrestin 实验中，IC50值分别为 0.70 μM 和 1.75 μM，EC80值均为 10 nM。
TP2158	TRV-120027 TFA TRV-120027 TFA (1234510-46-3 free base)	RAAS; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	TRV-120027 TFA 是一种血管紧张素 II 介导的血管收缩抑制剂，可增加心肌细胞的收缩力。它是一种偏向 β-arrestin-1 的 AT1R 激动剂，可与 ß-arrestins 结合，同时阻断 G 蛋白信号传导。它通过阳离子通道亚家族 C3 (TRPC3) 偶联诱导急性儿茶酚胺分泌，并促进在质膜上形成由 AT1R-β-arrestin-1-TRPC3-PLCγ 组成的大分子复合物。
TP1923L1	ELA-14(human) acetate ELA-14(human) acetate (1886973-05-2 free base)	Apelin receptor; Arrestin	GPCR/G Protein
	ELA-14(human) acetate 是 ELA 的一个片段，它与 APJ 结合，激活 Gαi1 和 β-arrestin-2 信号通路，并类似于其亲本内源性肽诱导受体内化。
TP1922L1	ELA-11 (human) acetate(1784687-32-6 free base)	Apelin receptor; Arrestin	GPCR/G Protein
	ELA-11 (human) acetate(1784687-32-6 free base)是亲和力 apelin 受体激动剂 (Ki = 14 nM)。 ELA-32 的生物活性片段。在体外抑制毛喉素诱导的 cAMP 产生并刺激 β-arrestin 募集。
TP2112L	TC14012 acetate TC14012 acetate(368874-34-4 free base)	CXCR; Arrestin	Autophagy; GPCR/G Protein; Immunology/Inflammation
	TC14012 acetate 是 T140 的血清稳定衍生物，是一种选择性的肽模拟 CXCR4 拮抗剂，IC50 为 19.3 nM。 TC14012 还是一种有效的 CXCR7 激动剂，EC50 为 350 nM，可将 β-arrestin 2 募集到 CXCR7。 TC14012 具有抗癌活性和抗 HIV 活性。
TP2158L1	TRV-120027 acetate (1234510-46-3 free base)	RAAS; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	TRV-120027 acetate (1234510-46-3 free base) 是 1 型血管紧张素 II 受体（AT1 受体）的 β-arrestin-1 偏向激动剂，可与 ß-arrestins 结合，同时阻断 G 蛋白信号传导。
T77673	7-FluorotryptaMine HCl	GPR; Arrestin	Endocrinology/Hormones; GPCR/G Protein
	7-FluorotryptaMine HCl 是一种有效的芳香单胺 GPRC5A 激动剂，可诱导 GPRC5A 介导的 β-arrestin 募集。7-FluorotryptaMine HCl 可用于研究与免疫和癌症相关的信号通路。
T41231	GP 1a	Cannabinoid Receptor; PERK; Arrestin	Apoptosis; GPCR/G Protein
	GP 1a 是cannabinoid receptor 2（CB2）的强效激动剂（EC50=7.1),是在cAMP、GTPγS 和β-arrestin 招募试验中显示的。GP 1a 对CB2受体的选择性约为CB1受体的30倍，且在体外增加HL-60细胞的P-ERK1/2表达。GP 1a 对皮肤伤口愈合有益。GP 1a 可抑制炎症和纤维生成，同时促进上皮的重新形成。
T33613	NCGC00135472 NCGC 00135472,DRV1 (GPR32) agonist C2A,C2A,NCGC-00135472	Others	Others
	NCGC00135472 (DRV1 (GPR32) agonist C2A)是具有促分解功能的人Resolvin D1受体激动剂,可在β阻滞素和 cAMP 测定中激活人溶解蛋白 D1 受体 DRV1/GPR32 受体，EC50 分别为 0.37 uM 和 0.05 uM。NCGC00135472在过表达重组DRV1的细胞中引起快速阻抗变化，刺激血清处理的酶聚糖的吞噬作用。
T29065	UNC9994 UNC-9994,UNC 9994
	UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities.
T29061	UNC0006 UNC 0006,UNC-0006
	UNC0006 is a β-arrestin-biased dopamine D2 ligand.
T29064	UNC9975 UNC-9975
	UNC9975 is an analog of aripiprazole and a β-arrestin-biased D2R agonist.
T29066	UNC9995 UNC-9995,UNC 9995
	UNC9995 is a β-Arrestin-Biased Dopamine D2 Receptor agonist (β-Arrestin, EC50 = 120 nM; Emax = 88%).
T61371	CB1R Allosteric modulator 4
	CB1R Allosteric modulator 4 is an effective and positive modulator of cannabinoid type-1 (CB1R), exhibiting significant biological activity. This compound inhibits the production of cAMP and demonstrates strong β-arrestin-2 recruitment [1].
T70040	BRD5814
	BRD5814 is a highly brain penetrant β-arrestin biased D2R antagonist.
T10926L	CYT-1010 hydrochloride	Others	Others
	CYT-1010 hydrochloride is an mu-opioid receptor agonist. The EC50 for β-arrestin recruitment and cAMP production inhibition were 13.1 nM and 0.0053 nM, respectively.
T23866	CCX777 CCX 777,CCX-777	Arrestin	GPCR/G Protein
	CCX777 是 β-arrestin-2 招募到 ACKR3 的部分激动剂,可用于研究癌症。
T79312	FGH31	Dopamine Receptor	GPCR/G Protein; Neuroscience
	FGH31 (Compound 24) 作为选择性GRK2依赖的dopamine D4激动剂，显示出Ki值为1.6 nM的高亲和力，并能部分激活β-arrestin。
T37304	5-OxoETE methyl ester
	5-OxoETE methyl ester is an esterified form of the polyunsaturated keto acid 5-oxoETE . 5-OxoETE methyl ester is an agonist of oxoeicosanoid receptor 1 (OXER1; EC50 = 1.54 μM for β-arrestin recruitment) that has a higher maximal response than 5-oxoETE in a β-arrestin assay.
T78736	D3R ligand 1	Dopamine Receptor	GPCR/G Protein; Neuroscience
	D3R ligand 1 (compound 23b) 是针对多巴胺受体D3R具有高效选择性的配体，拥有66 nM的Ki值，且包含THPB模板。此外，D3R ligand 1 同时作为基于G蛋白及β-arrestin信号传导路径的拮抗剂。
T10926	CYT-1010	Others	Others
	CYT-1010 is an mu-opioid receptor agonist. The EC50 for the inhibition of β-arrestin recruitment and cAMP production is 13.1 nM and 0.0053 nM, respectively.
T80140	(Val3,Pro8)-Oxytocin	Oxytocin Receptor	Endocrinology/Hormones; GPCR/G Protein
	"(Val3,Pro8)-Oxytocin"为Gq依赖性途径的激动剂，同时作为β-arrestin结合及催产素受体（OXTR）内化作用的次级激动剂。
T62853	UNC9994 hydrochloride
	UNC9994 hydrochloride 是一种功能选择性的、β-arrestin 偏向的多巴胺 D2受体 (D2R) 激动剂 (Ki: 79 nM)，能够选择性激活 β- arresttin 招募和信号转导。UNC9994 hydrochloride 是一种 Gi 调节 cAMP 产生的拮抗剂，也是 D2R/β-arrestin-2 相互作用的部分激动剂，表现出精神稳定作用。
TP2158L	TRV-120027	Others	Others
	TRV120027 is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1. TRV120027 inhibits angiotensin II-mediated vasoconstriction and increases cardiomyocyte contractility.
T79744	GPR55 agonist 4
	GPR55agonist 4 (Compound 28)，作为一种高选择性激动剂，对hGPR55 和 rGPR55 的EC50值分别为131 nM和1.41 nM，能有效诱导β-arrestin招募至人GPR55。
T70342	MRS542
	MRS542 is a A3AR antagonist as found by cyclic AMP assays, and a partial agonist as found by beta-arrestin translocation. LUF6000 is responsible for the partial agonist nature of MRS542.
T68247	PSB-KD107
	PSB-KD107 is an agonist of the Cannabinoid-Activated Orphan G‑Protein-Coupled Receptor GPR18. PSB-KD107 displayed significantly higher potency and efficacy than THC, determined in a GPR18-dependent β-arrestin recruitment assay, and were found to be selective versus the CB-sensitive receptors CB1, CB2, and GPR55.
T61964	RXFP3/4 agonist 2	RXFP receptor	GPCR/G Protein
	RXFP3/4 agonist 2 是一种高效的非肽双 RXFP3/4 激动剂，诱导 RXFP3 和 β-arrestin-2 之间的相互作用，可用于研究代谢异常引起的疾病。
T79721	GPR55 agonist 3
	GPR55agonist 3 (Compound 26)作为一种高效GPR55激动剂，其EC50值针对hGPR55与rGPR55分别为0.239 nM和1.76 nM。此外，该化合物在EC50为6.2 nM的条件下可诱导β-arrestin招募至人类GPR55。
T64305	APJ receptor agonist 7
	APJ receptor agonist 7 (化合物 37) 是一种口服具有活力的 APJ (apelin 受体) 激动剂 (Ki: 0.059 μM)。APJ receptor agonist 7 能够作用于钙 (EC50: 0.070 μM)、cAMP (EC50: 0.097 μM) 和 β-arrestin (EC50: 0.063 μM)。
T78735	D1R antagonist 1	Dopamine Receptor	GPCR/G Protein; Neuroscience
	D1R antagonist 1 (compound 12a)，一种参与基于G蛋白和β-抑制蛋白的信号传导的D1R拮抗剂。
T10716	CCR7 Ligand 1 CCR7-Cmp2105	Others	Others
	CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM
TP1922	ELA-11(human) ELA-11 (human)
	High affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
T76053	ELA-11(human) TFA
	ELA-11(human) TFA is a high affinityapelin receptoragonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
TP1923	Elabela(19-32) ELA-14 (human)
	Potent apelin (APJ) receptor agonist (Ki = 0.93 nM). Bioactive fragment of ELA-32. Activates Gαi1 pathway and β-arrestin-2 recruitment. Reduces arterial pressure in rat hearts. Active in vivo.
T76044	Elabela(19-32) TFA
	Elabela(19-32) TFA 是ELABELA（ELA）与apelin受体(APJ)结合的活性片段，能激活Gαi1和β-arrestin-2信号通路，EC50值分别为8.6 nM和166 nM。该化合物可诱导受体内在化，降低动脉压，并对心脏具有正性肌力作用。
T73690	Abaloparatide
	Abaloparatide (BA 058) 是一种甲状旁腺激素受体 1 (PTHR1) 类似物。Abaloparatide 也是一种选择性 PTHR1激活剂。Abaloparatide 增强 Gs/cAMP 信号和β-arrestin 募集。Abaloparatide 可增强小鼠的骨形成和皮质结构。Abaloparatide 具有用于骨质疏松症研究的潜力。
T69824	PSB-17365
	PSB-17365 is a potent GPR84 agonist. PSB-17365 exhibits EC50 values vs. GPR84 of 2.5nM in a cAMP accumulation assay, and 100nM in a β-arrestin 2 recruitment assay. No direct binding affinities are provided. PSB-17365 is selective for GPR84 compared to other free fatty acid receptors (FFAR1 and FFAR4). GPR84, a Gi protein-coupled receptor that is activated by medium-chain (hydroxy)fatty acids, appears to play an important role in inflammation, immunity, and cancer.
TP2141	Balixafortide TFA (1051366-32-5 free base) Balixafortide TFA,POL6326 TFA	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Balixafortide TFA (POL6326 TFA) is a selective, well-tolerated peptidic CXCR4 antagonist (IC50 < 10 nM). It shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium fl
T14498	Barbadin	Arrestin	GPCR/G Protein
	Barbadin 是一种新型且具有特异性的 β-arrestin/β2-adaptin 相互作用抑制剂，对β-arestin1 的 IC50 值为 19.1 μM，对β-arestin2 的 IC50 值为 15.6 μM。Barbadin 增强氯卡色林对 POMC 神经元和减肥的长期影响，可阻断激动剂促进的原型 β2-肾上腺素能、V2-血管加压素和血管紧张素-II-1 型受体的内吞，可用于研究肥胖。
T36923	CXCR2-IN-2 CXCR2-IN-2
	CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM[1]. CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in ra...

化合物

Cat.No: T21874

Target: GPR

Cat.No: T8423

Target: Dopamine Receptor, Arrestin

Cat.No: T26869

Synonym: BMS 986122

Target: Opioid Receptor

Cat.No: T28073

Synonym: MLS000051547,MLS 1547,MLS-1547

Target: Dopamine Receptor

Cat.No: T12006

Synonym: ML246

Target: DNA/RNA Synthesis

Cat.No: T15183

Target: Hedgehog/Smoothened

CB1R Allosteric modulator 3

Cat.No: T61562

Target: cAMP, Cannabinoid Receptor

GPR35 agonist 2

Cat.No: T23434

Synonym: TC-G 1001

Target: GPR, Arrestin

Cat.No: T33452

Synonym: ML-192,CID1434953,CID 1434953,ML 192,CID-1434953

Target: Cannabinoid Receptor, GPR, Arrestin

Cat.No: T4390

Target: Apelin receptor, Arrestin

Cat.No: TP2158

Synonym: TRV-120027 TFA (1234510-46-3 free base)

Target: RAAS, Arrestin

ELA-14(human) acetate

Cat.No: TP1923L1

Synonym: ELA-14(human) acetate (1886973-05-2 free base)

Target: Apelin receptor, Arrestin

ELA-11 (human) acetate(1784687-32-6 free base)

Cat.No: TP1922L1

Target: Apelin receptor, Arrestin

TC14012 acetate

Cat.No: TP2112L

Synonym: TC14012 acetate(368874-34-4 free base)

Target: CXCR, Arrestin

TRV-120027 acetate (1234510-46-3 free base)

Cat.No: TP2158L1

Target: RAAS, Arrestin

7-FluorotryptaMine HCl

Cat.No: T77673

Target: GPR, Arrestin

Cat.No: T41231

Target: Cannabinoid Receptor, PERK, Arrestin

Cat.No: T33613

Synonym: NCGC 00135472,DRV1 (GPR32) agonist C2A,C2A,NCGC-00135472

Target: Others

Cat.No: T29065

Synonym: UNC-9994,UNC 9994

Cat.No: T29061

Synonym: UNC 0006,UNC-0006

Cat.No: T29064

Synonym: UNC-9975

Cat.No: T29066

Synonym: UNC-9995,UNC 9995

CB1R Allosteric modulator 4

Cat.No: T61371

Cat.No: T70040

CYT-1010 hydrochloride

Cat.No: T10926L

Target: Others

Cat.No: T23866

Synonym: CCX 777,CCX-777

Target: Arrestin

Cat.No: T79312

Target: Dopamine Receptor

5-OxoETE methyl ester

Cat.No: T37304

Cat.No: T78736

Target: Dopamine Receptor

Cat.No: T10926

Target: Others

(Val3,Pro8)-Oxytocin

Cat.No: T80140

Target: Oxytocin Receptor

UNC9994 hydrochloride

Cat.No: T62853

Cat.No: TP2158L

Target: Others

GPR55 agonist 4

Cat.No: T79744

Cat.No: T70342

Cat.No: T68247

RXFP3/4 agonist 2

Cat.No: T61964

Target: RXFP receptor

GPR55 agonist 3

Cat.No: T79721

APJ receptor agonist 7

Cat.No: T64305

D1R antagonist 1

Cat.No: T78735

Target: Dopamine Receptor

Cat.No: T10716

Synonym: CCR7-Cmp2105

Target: Others

Cat.No: TP1922

Synonym: ELA-11 (human)

ELA-11(human) TFA

Cat.No: T76053

Cat.No: TP1923

Synonym: ELA-14 (human)

Elabela(19-32) TFA

Cat.No: T76044

Cat.No: T73690

Cat.No: T69824

Balixafortide TFA (1051366-32-5 free base)

Cat.No: TP2141

Synonym: Balixafortide TFA,POL6326 TFA

Target: CXCR

Cat.No: T14498

Target: Arrestin

Cat.No: T36923

Synonym: CXCR2-IN-2

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