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Cat. No.	Product Name	Target	Signaling Pathways
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。
TQ0075	ML314	Neurotensin Receptor	GPCR/G Protein
	ML314 是一种具有脑渗透性非肽 β-抑制素偏向神经降压素 NTR1 受体激动剂（EC50：1.9 μM），是一种用于甲基苯丙胺滥用的偏向神经降压素受体配体，抑制 NTR2 和 GPR35。
T23002	ML-335	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	ML-335 是μ-δ异构体靶向激动剂，是一种μOR-δOR 偏向配体，可以作为开发独特类型（异构体偏倚）药物的支架。ML-335是MOR（μ阿片受体）/DOR（δ阿片受体）异构体，具有抗伤害感受活性和抑制疼痛的活性。
T40508L	TRV120056 acetate TRV120056 acetate (40678-47-5 Free base)	Others	Others
	TRV120056 acetate 是一种 Gq 偏向激动剂，对 AT1R-Gq 融合蛋白的分子效率比 AT1R-βarr2 融合蛋白高 10 倍。
T7281	F-15599	5-HT Receptor	GPCR/G Protein; Neuroscience
	F-15599 是一种高度选择性的 G 蛋白偏向 5-HT1A 受体激动剂，Ki 值为 3.4 nM。
T9596	AP1189 acetate	Melanocortin Receptor	GPCR/G Protein; Neuroscience
	AP1189 acetate 是黑皮质素 1 和黑皮质素 3 受体的偏向激动剂。
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。
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。
T16321	NI-42	Epigenetic Reader Domain	Chromatin/Epigenetic
	NI-42 是一种用于 BRPF 的结构正交化学探针，是有偏向性的BRPFs 溴结构域 (BRD)抑制剂，BRPF1、2和3的IC50为7.9、48和260 nM; BRPF1、2和3的Kd 值为40、210和940 nM，与非分类 IV BRD 蛋白相比具有很好的选择性。
T71946	ID110460003
	ID110460003 is a novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist.
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%).
T70040	BRD5814
	BRD5814 is a highly brain penetrant β-arrestin biased D2R antagonist.
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.
T40508	TRV120056
	TRV120056 is a Gq-biased agonist that demonstrates a molecular efficacy ten times greater at the AT1R-Gq fusion protein than at the AT1R-βarr2 fusion protein.
T40220	TRV055 TRV055
	TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
T40920	TRV056 TRV056
	TRV056 is a Gq-biased agonist of the angiotensin II type 1 receptor (AT1R), demonstrating efficacy in stimulating Gq-mediated cellular signaling. It can serve as a foundation for the development of Gq-biased AT1R agonists.
T71438	ID110460001
	ID110460001 is a novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist.
T71985	ID110460002
	ID110460002 is a novel μ,δ-Opioid Receptor Dual-Biased Agonist, Overcoming the Limitation of Prior Biased Agonist.
T60790	5-HT7R antagonist 1
	5-HT7R antagonist 1 是一种 G 蛋白偏向性的拮抗剂，对5-HT7R 的 Ki 值为6.5 nM。
T69844	NLX-219
	NLX-219 is a selective 5-HT1A receptor-biased agonists.
T70765	TRV0109101
	TRV0109101 is a G protein-biased agonist of the µ-opioid receptor.
T39870	5-HT7R antagonist 1 free base 5-HT7R antagonist 1 free base
	5-HT7R antagonist 1 (free base) is a G protein-biased antagonist for the 5-HT 7 R receptor, with a dissociation constant (K i) of 6.5 nM.
T39995	TRV120055 TRV120055
	TRV120055, a Gq-biased agonist, demonstrates a 10-fold higher molecular efficacy when tested against the AT1R-Gq fusion protein in comparison to the AT1R-βarr2 fusion protein.
T76196	TRV055 hydrochloride
	TRV055 hydrochloride，G 蛋白-偏向激动剂，作为AT1R的Gq-偏向配体，有效激发细胞内Gq介导信号传导。
T36946	PW0464 PW0464
	PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1]. PW0464 (compound 24) is found to elicit complete G protein bias, showing no activity for D1R-mediated β-arrestin recruitment[1].PW0464 (compound 24), the non-catechol agonist, forms bonds with S1985.42 and S2025.46 via its fluorine atom[2]. [1]. Pingyuan Wang, et al. Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Recept...
T37622	F13714 fumarate F13714 fumarate
	F13714 fumarate, a selective biased agonist of the 5-HT1A receptor, exhibits antidepressant-like effects upon single administration in the mouse model of chronic mild stress[1].
TP2000	MM 07
	Apelin biased agonist; exhibits bias for the G protein pathway. Stimulates endothelial NOS phosphorylation and expression, promotes proliferation, and attenuates apoptosis of human pulmonary arterial endothelial cells in vitro. Shows positive inotropic an
T37907	DL 175
	Potent and selective GPR84 biased agonist (EC50 = 33 nM). Exhibits no significant activity in a panel of 168 other GPCRs. Exhibits bias for G protein signaling pathways. Induces morphological changes in primary murine bone marrow-derived macrophages (BMDMs) in a cellular impedance assay, and promotes phagocytosis by M1 polarized U937 cells. Induces migration of primary human monocytes, but has no effect on macrophage chemotaxis.
T41189	AY 254
	AY 254 is a potent PAR2 biased agonist. Selectively activates ERK1/2 signaling (EC50= 2 nM for ERK1/2 phosphorylation versus 80 nM for Ca2+release). Reduces cytoKi ne-induced caspase 3/8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cellsin vitro.
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.
T38716	SAR247799 SAR247799,S1P1 agonist 3
	SAR247799 (S1P1 agonist 3) is an orally-active, selective G-protein-biased agonist for the sphingosine-1 phosphate receptor-1 (S1P1). It demonstrates EC50 values ranging from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 holds promise as a valuable tool for investigating endothelial protection, particularly in the context of type-2 diabetes and metabolic syndrome[4].
T76224	NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)
	NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (化合物40) 作为 Ape13 的大环类似物，是一种 APJ 强效激动剂，具有较低的亲和力 (Ki=5.7 nM)。该化合物在 Gα12 路线上显示出优先的信号传递特性，并且在体内具有延长的半衰期。
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。
TP1354	ATI-2341 TFA (1337878-62-2 free base) ATI-2341 TFA
	ATI-2341 is an effective functionally selective allosteric agonist for the c-x-c chemokine receptor type 4 (CXCR4), which ACTS as a biased ligand in favor of G G G G G 1 activation instead of G G G G G 13.ATI-2341 activates the inhibitory heterotrimer G p
T60597	UCSF678
	UCSF678 是一种 42 nM 抑制蛋白偏向的5-HT5AR 部分激动剂，与单一商业拮抗剂 SB-699551 相比，具有更受限制的脱靶特征和降低的检测倾向。UCSF678是一种选择性探针，可用于研究 5-HT5AR 的功能。
T80471	α-Conotoxin MrIC
	α-Conotoxin MrIC为特异性α7nAChR偏向激动剂，仅针对II型正变构调节剂（例如PNU120596）调控的α7nAChR产生激活作用。该化合物适用于神经系统疾病研究，以及α7nAChR药理特性的探测。
T82233	HCAR2 agonist 1
	HCAR2 agonist 1 (Compound 9n) 是一种偏向Gi蛋白的变构调节剂，能够激活Gi蛋白相关的信号传导通路。该化合物展现了明显的抗炎效果，能够显著降低促炎细胞因子（TNF-α、IL-1β、IL-6 和 MCP-1）的mRNA表达水平，并在结肠炎小鼠模型中增强正位激动剂的抗炎作用。
T75721	ATI-2341 TFA
	ATI-2341是一种针对C-X-C趋化因子受体4型(CXCR4)的功能选择性变构激动剂，作为偏向配体，偏好促进Gα1而不是Gα13的激活。通过激活抑制性异源三聚体G蛋白(Gi)，ATI-2341抑制cAMP的产生并诱导钙动员，有效动员骨髓多形核中性粒细胞(PMNs)与造血干细胞及其祖细胞(HSPCs)。
T37199	Bilaid C
	Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Siana...

化合物

Cat.No: T28073

Synonym: MLS000051547,MLS 1547,MLS-1547

Target: Dopamine Receptor

Cat.No: TQ0075

Target: Neurotensin Receptor

Cat.No: T23002

Target: Opioid Receptor

TRV120056 acetate

Cat.No: T40508L

Synonym: TRV120056 acetate (40678-47-5 Free base)

Target: Others

Cat.No: T7281

Target: 5-HT Receptor

Cat.No: T9596

Target: Melanocortin Receptor

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

Cat.No: TP2158L1

Target: RAAS, Arrestin

Cat.No: TP2158

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

Target: RAAS, Arrestin

Cat.No: T16321

Target: Epigenetic Reader Domain

Cat.No: T71946

Cat.No: T29061

Synonym: UNC 0006,UNC-0006

Cat.No: T29064

Synonym: UNC-9975

Cat.No: T29066

Synonym: UNC-9995,UNC 9995

Cat.No: T70040

Cat.No: T29065

Synonym: UNC-9994,UNC 9994

Cat.No: T40508

Cat.No: T40220

Synonym: TRV055

Cat.No: T40920

Synonym: TRV056

Cat.No: T71438

Cat.No: T71985

5-HT7R antagonist 1

Cat.No: T60790

Cat.No: T69844

Cat.No: T70765

5-HT7R antagonist 1 free base

Cat.No: T39870

Synonym: 5-HT7R antagonist 1 free base

Cat.No: T39995

Synonym: TRV120055

TRV055 hydrochloride

Cat.No: T76196

Cat.No: T36946

Synonym: PW0464

F13714 fumarate

Cat.No: T37622

Synonym: F13714 fumarate

Cat.No: TP2000

Cat.No: T37907

Cat.No: T41189

Cat.No: TP2158L

Target: Others

Cat.No: T38716

Synonym: SAR247799,S1P1 agonist 3

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)

Cat.No: T76224

UNC9994 hydrochloride

Cat.No: T62853

ATI-2341 TFA (1337878-62-2 free base)

Cat.No: TP1354

Synonym: ATI-2341 TFA

Cat.No: T60597

α-Conotoxin MrIC

Cat.No: T80471

HCAR2 agonist 1

Cat.No: T82233

Cat.No: T75721

Cat.No: T37199

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