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105

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40685L	Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (600171-70-8 Free base)	Others	Others
	Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (Orphan GPCR SP9155 agonist P550 ) 是具有促食欲作用的 RFamide 肽家族的成员。
T40685	Orphan GPCR SP9155 agonist P550 (mouse, rat) 26RFa (mouse, rat),Orphan GPCR SP9155 agonist P550 (mouse, rat)
	Orphan GPCR SP9155 agonist P550 (mouse, rat) (26RFa (mouse, rat)) is an orphan GPCR with an orexigenic effect belonging to the RFamide peptide family. It acts as the cognate ligand for the mouse orphan receptor GPR103, which is also known as SP9155 or AQ27.
T16832	S18-000003	ROR	Metabolism
	S18-000003 是口服有活性的维甲酸相关孤儿受体 (RORγt) 选择性抑制剂，在竞争性结合试验中，对 hRORγt 的 IC50值小于 30 nM。它对 RORγt 的选择性比其他 ROR 家族成员 (IC50>10 μM)更高。它可用于银屑病的研究，胸腺畸变风险较低。
T39250	Bevurogant	ROR	Metabolism
	Bevurogant 是 RORγt 受体的拮抗剂，可用于治疗慢性炎症性疾病的研究。
T5163	SR1001	ROR	Metabolism
	SR1001 是选择性RORα及RORγt 的反向激动剂，其Ki 分别为 172 和 111 nM。
T4670	SR0987	ROR	Metabolism
	SR0987是SR1078 的类似物，是RORγt 的激动剂，其EC50=800 nM。它可上调IL17 的表达，并且抑制PD-1 的表达。
TQ0007	Cintirorgon LYC-55716	ROR	Metabolism
	Cintirorgon (LYC-55716) 是一种首创的、口服有活力的的RORγ选择性激动剂。它通过调节 RORγ 表达的 T 淋巴免疫细胞的基因表达，提高效应子功能，降低免疫抑制，抑制肿瘤生长，提高生存率。
T4594	SR1078 SR 1078	ROR	Metabolism
	SR1078 是视黄酸受体相关孤儿受体 (RORα/RORγ) 激动剂。它能够与 RORα 和 RORγ 的配体结合区直接结合，增强该受体的转录活性，促使 RORα/γ 靶基因的转录。
T7388	GSK805	ROR	Metabolism
	GSK805 是能够生物利用的、具有 CNS 穿透性的 RORγt 抑制剂。
T7833	TLX agonist 1	Others	Others
	TLX agonist 1 是一种孤核受体tailless (TLX, NR2E1)调节剂 (EC50=1 μM;Kd= 650 nM)。它能够提高 TLX 转录抑制活性。
T9635	Cedirogant ABBV-157	ROR	Metabolism
	Cedirogant (ABBV-157) 是一种口服有活性的 RORγt 反向激动剂，可用于研究银屑病。
T14369	AZD-0284	ROR	Metabolism
	AZD-0284 是核受体 (RORγ) 的选择性反向激动剂。它对呼吸道疾病及斑块型寻常型银屑病具有潜在的应用价值。
T9623	RORγt inverse agonist 13	ROR	Metabolism
	RORγt inverse agonist 13 是一种口服有效的RORγt 选择性反向激动剂，IC50为 63.8 nM。
T5160	SR3335 ML 176	ROR	Metabolism
	SR3335 (ML 176) 是特异性RORα反向激动剂，能够与 RORα直接结合，其Ki=220 nM。
T12753	RORγt Inverse agonist 6	ROR	Metabolism
	RORγt Inverse agonist 6 是 RORγt inverse 的激动剂。 RORγt Inverse agonist 6 可用于研究 Th17 驱动的自身免疫性疾病。
T4050	GSK2981278 ROR gama modulator 1	ROR	Metabolism
	GSK2981278 (ROR gama modulator 1) 是 RORγ的选择性反向激动剂。它能够抑制 il17启动子的激活，并且干扰 RORγ-DNA 结合。
T23204	PSN 375963 PSN 375963 hydrochloride	GPR	Endocrinology/Hormones; GPCR/G Protein
	PSN 375963 (PSN 375963 hydrochloride) hydrochloride 是GPR119激动剂，对人和小鼠的EC50分别为 8.4 和 7.9 μM。它表现出与内源性油酰乙醇酰胺 (OEA) 相似的效力。
T12075	ML-180 SR1848	Others	Others
	ML-180 (SR1848) 是孤儿核受体肝受体同源物 1 (LRH-1;NR5A2) 的反向激动剂(IC50:3.7 µM)。它不抑制类固醇生成因子 1 (SF-1;NR5A1; IC50>10 µM)。它具有潜在的抗依赖 LRH-1 癌症作用。
T6690	T0901317 N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]苯磺酰胺	Apoptosis; FXR; Liver X Receptor; ROR	Apoptosis; Metabolism
	T0901317 是一种口服有效且高度选择性的LXR 激动剂，对 LXRα 的EC50为 20 nM。它激活FXR，EC50为 5 μM。它是RORα和RORγ双重反向激动剂，Ki 值分别为 132 nM 和 51 nM。它诱导细胞凋亡，并抑制低密度脂蛋白受体缺失小鼠动脉粥样硬化的发展。
T67888L	Samidorphan HCl Samidorphan HCl（852626-89-2 free base）	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Samidorphan HCl 是一种具有口服活性和高效性的 opioid 系统调节剂，可与 μ‐opioid、 κ‐opioid 和 δ‐opioid 受体结合。Samidorphan HCl 是一种新型 μ‐opioid 受体拮抗剂，是 k-opioid 受体和 δ‐opioid 受体的部分激动剂。Samidorphan HCl 可用于预防和治疗精神分裂。
TP1882L1	Orphanin FQ(1-11) acetate(178249-41-7 free base)	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Orphanin FQ(1-11) acetate(178249-41-7 free base) 含有 Nociceptin 氨基酸 1-11 的肽片段。 ORL1/KOR-3 受体的强效激动剂 (Ki = 55 nM)；对阿片受体无亲和力，包括 μ、δ、κ1 和 κ3 受体 (Ki >1000 nM)。在 CD-1 小鼠中显示镇痛特性。
T7693	Thiorphan	Neprilysin	Metabolism
	Thiorphan 是选择性neprilysin 抑制剂 (IC50:6.9 nM) 。
T69060	Dextrallorphan
	Dextrallorphan (DXA) is an chemical of the morphinan class that is used in scientific research. It acts as a σ1 receptor agonist and NMDA receptor antagonist. It has no significant affinity for the σ2, μ-opioid, or δ-opioid receptor, or for the serotonin or norepinephrine transporter. As an NMDA receptor antagonist, in vivo, it is approximately twice as potent as dextromethorphan, and five-fold less potent than dextrorphan. Dextrallorphan was found to have a half maximal inhibitory concentration...
T25690	Levallorphan tartrate Lorfan
	Levallorphan tartrate is an opioid antagonist with properties similar to those of NALOXONE. Levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid ce
T35185	Xorphanol TR-5379,TR5379,TR 5379
	Xorphanol is a biochemical.
T70964	Olanzapine/Samidorphan
	Olanzapine/Samidorphan is a combination of olanzapine and the opioid receptor antagonist samidorphan is under development for the treatment of schizophrenia and bipolar I disorder. The single-tablet combination treatment is intended to provide the efficacy of olanzapine while mitigating olanzapine-associated weight gain.
T25941	Phelorphan
	Phelorphan is an inhibitor of enkephalinase.
T25676	Leucine thiorphan Leu-thiorphan
	Leucine thiorphan is an inhibitor of enkephalinase.
T15652	Kelatorphan	Others	Others
	Kelatorphan is an enkephalin degrading enzyme full inhibitor.
T68601	Azidothiorphan
	Azidothiorphan is a photoaffinity ligand for the active site of the neutral endopeptidase 24.11. After ultraviolet irradiation the inhibitor binds irreversibly to the enzyme, and photolabeling occurs at the active site. The competitive inhibitor thiorphan protects the endopeptidase from inactivation.
T71161	Thiorphan disulfide
	Thiorphan disulfide is an impurity of Racecadotril -- an antidiarrheal and enkephalinase inhibitor that reduces the amount of water and electrolytes absorbed into the intestine.
T35185L	Xorphanol mesylate TR 5379M,TR5379M,TR-5379M
	Xorphanol mesylate is a biochemical.
T67888	Iso-Samidorphan (9ξ,13ξ,14ξ)-17-(Cyclopropylmethyl)-4,14-dihydroxy-6-oxomorphinan-3-carboxamide	Others	Others
	Iso-Samidorphan 是一种生化试剂，可用于生物实验。
T75897	Orphanin FQ(1-11) TFA
	Orphanin FQ(1-11) TFA 是孤儿蛋白 FQ 或 nociceptin (OFQ/N) 片段，是一种有效的NOP 受体 (ORL-1; OP4) 激动剂，Ki 为 55 nM。Orphanin FQ(1-11) TFA 对 μ，δ，κ1 和 κ3 受体没有亲和力 (Ki>1000 nM)。Orphanin FQ(1-11) TFA 在 CD-1 小鼠中具有缓解疼痛作用。
T32690	Levallorphan Levallorphanum,Lorfan,Levallorphane,Levalorfano,Naloxiphan
	Levorphane (levorphane tartrate) is an opioid modulator of the Morphan family that acts as an antagonist for μ-opioid receptor (MOR) and an agonist for κ-opioid receptor (KOR).
TP1882	Orphanin FQ(1-11) Orphanin FQ (1-11)
	Orphanin FQ(1-11) is a peptide fragment containing amino acids 1-11 of Nociceptin. Orphanin FQ(1-11) is a potent agonist of the ORL1/KOR-3 receptor (Ki = 55 nM) and displays no affinity for opioid receptors, including μ, δ, κ1 and κ3 receptors (Ki >1000 nM). Orphanin FQ(1-11) displays analgesic properties in CD-1 mice.
T25910	Oxilorphan Oxilorfano,Oxilorphane,Bristol laboratories BC 2605,levo-BC-2605
	Oxilorphan acts as a μ-opioid receptor (MOR) antagonist but a κ-opioid receptor (KOR) partial agonist and has similar effects to naloxone and around the same potency as a MOR antagonist. Oxilorphan has some weak partial agonist actions at the MOR and can
T60074	GPCR agonist-2 4-(Cyclopropylamino)-3-nitrobenzoic acid	GPR	Endocrinology/Hormones; GPCR/G Protein
	GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) 是人源 GPCR GPR109B 的激动剂。
TP2165	Urotensin II, mouse acetate (9047-55-6 free base) Urotensin II, mouse acetate	GPR	Endocrinology/Hormones; GPCR/G Protein
	Urotensin II, mouse acetate (9047-55-6 free base) 是孤儿 GPR14 或 SENR 的内源性配体。它是一种强效血管收缩剂。
TP1737L	Urotensin II (114-124), human acetate Urotensin II (114-124), human acetate(251293-28-4 free base)	GPR	Endocrinology/Hormones; GPCR/G Protein
	Urotensin II (114-124), human acetate(251293-28-4 free base) 是一种 11 个氨基酸残基肽，是一种有效的血管收缩剂和孤儿受体 GPR14 的激动剂。
T39823L	Apelin-12 acetate Apelin-12 acetate (229961-08-4 Free base)	Apelin receptor; p38 MAPK; JNK	GPCR/G Protein; MAPK
	Apelin-12 acetate 对 APJ 受体具有高亲和力。 Apelin-12 acetate 抑制凋亡相关 MAPKs 家族的 JNK 和 p38 MAPK 信号通路，从而为神经元提供保护。
TP2073L	BigLEN (mouse) acetate BigLEN (mouse) acetate (501036-69-7 Free base)	GPR	Endocrinology/Hormones; GPCR/G Protein
	BigLEN (mouse) acetate 是一种有效的、选择性的孤儿 G 蛋白偶联受体 171 (GPR171) 激动剂，Kd 为 ~0.5 nM。
T5422	CID 1375606 CID-1375606,CID1375606	Others	Others
	CID 1375606 是孤儿 G 蛋白偶联受体GPR27的代理激动剂。
T60199	NCRW0005-F05	GPR	Endocrinology/Hormones; GPCR/G Protein
	NCRW0005-F05 是一种有效的孤儿 G 蛋白偶联受体GPR139的激动剂，IC50为 0.21 μM。NCRW0005-F05 可用于研究糖尿病、肥胖症和帕金森的研究。
T13586L	BPK-29 hydrochloride	Others	Others
	BPK-29 hydrochloride 是特殊配体，能够共价修饰 C274 ，破坏非典型孤核受体NR0B1与RBM45、SNW1蛋白质的相互作用。它能够损害KEAP1突变癌细胞的锚定独立生长。
T0755	Carglumic Acid Carbaglu,N-Carbamylglutamate,N-Carbamyl-L-glutamic acid,氨甲酰谷氨酸,Carbamylglutamic acid,Carbamino-L-glutamic acid,Ureidoglutaric acid	Others	Others
	Carglumic Acid (Ureidoglutaric acid) 是一种 N-乙酰谷氨酸 (NAG) 的功能类似物和氨甲酰磷酸合成酶 1(CPS1)的活化剂，可用于与 N-乙酰谷氨酸合成酶 (NAGS) 缺陷相关的急性和慢性高氨血症的研究。
TP1982L	Neuropeptide S (Rat) acetate	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	Neuropeptide S (Rat) acetate 是以前孤儿 G 蛋白偶联受体的内源性配体，现在称为 NPS 受体。它可用于神经系统疾病的研究。
T19700	IBC 293 IBC293,1-异丙基-1H-1,2,3-苯并噻唑-5-羧酸,IBC-293	GPR	Endocrinology/Hormones; GPCR/G Protein
	IBC 293 对 GPR109B 的选择性高于烟酸受体 GPR109A。 IBC 293 是 GPR109B 的高选择性激动剂，GPR109B 是一种在脂肪细胞中表达的人类孤儿 G 蛋白偶联受体。
T67694	ZY-19489	Parasite	Microbiology/Virology
	ZY-19489是一种具有抗疟作用的化合物，是一种潜在的单剂量根治性恶性疟原虫和间日疟原虫疟疾的药物，已获得美国 FDA 的孤儿药认定。
T37587	ML 209	ROR	Metabolism
	ML-209 是一种视黄酸相关的孤儿受体 RORγ 拮抗剂 (IC50= 1.1 μM)。ML-209 抑制 HEK293t 细胞中 RORγt 转录活性(IC50= 300 nM)。ML-209 不抑制细胞中 RORα。ML-209 对鼠 Th17 细胞分化具有选择性抑制，而不影响幼稚 CD4+ T 细胞分化为 Th1 和调节性 T 细胞。

化合物

Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate

Cat.No: T40685L

Synonym: Orphan GPCR SP9155 agonist P550 (mouse, rat) acetate (600171-70-8 Free base)

Target: Others

Orphan GPCR SP9155 agonist P550 (mouse, rat)

Cat.No: T40685

Synonym: 26RFa (mouse, rat),Orphan GPCR SP9155 agonist P550 (mouse, rat)

Cat.No: T16832

Target: ROR

Cat.No: T39250

Target: ROR

Cat.No: T5163

Target: ROR

Cat.No: T4670

Target: ROR

Cat.No: TQ0007

Synonym: LYC-55716

Target: ROR

Cat.No: T4594

Synonym: SR 1078

Target: ROR

Cat.No: T7388

Target: ROR

Cat.No: T7833

Target: Others

Cat.No: T9635

Synonym: ABBV-157

Target: ROR

Cat.No: T14369

Target: ROR

RORγt inverse agonist 13

Cat.No: T9623

Target: ROR

Cat.No: T5160

Synonym: ML 176

Target: ROR

RORγt Inverse agonist 6

Cat.No: T12753

Target: ROR

Cat.No: T4050

Synonym: ROR gama modulator 1

Target: ROR

Cat.No: T23204

Synonym: PSN 375963 hydrochloride

Target: GPR

Cat.No: T12075

Synonym: SR1848

Target: Others

Cat.No: T6690

Synonym: N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]苯磺酰胺

Target: Apoptosis, FXR, Liver X Receptor, ROR

Samidorphan HCl

Cat.No: T67888L

Synonym: Samidorphan HCl（852626-89-2 free base）

Target: Opioid Receptor

Orphanin FQ(1-11) acetate(178249-41-7 free base)

Cat.No: TP1882L1

Target: Opioid Receptor

Cat.No: T7693

Target: Neprilysin

Cat.No: T69060

Levallorphan tartrate

Cat.No: T25690

Synonym: Lorfan

Cat.No: T35185

Synonym: TR-5379,TR5379,TR 5379

Olanzapine/Samidorphan

Cat.No: T70964

Cat.No: T25941

Leucine thiorphan

Cat.No: T25676

Synonym: Leu-thiorphan

Cat.No: T15652

Target: Others

Cat.No: T68601

Thiorphan disulfide

Cat.No: T71161

Xorphanol mesylate

Cat.No: T35185L

Synonym: TR 5379M,TR5379M,TR-5379M

Iso-Samidorphan

Cat.No: T67888

Synonym: (9ξ,13ξ,14ξ)-17-(Cyclopropylmethyl)-4,14-dihydroxy-6-oxomorphinan-3-carboxamide

Target: Others

Orphanin FQ(1-11) TFA

Cat.No: T75897

Cat.No: T32690

Synonym: Levallorphanum,Lorfan,Levallorphane,Levalorfano,Naloxiphan

Orphanin FQ(1-11)

Cat.No: TP1882

Synonym: Orphanin FQ (1-11)

Cat.No: T25910

Synonym: Oxilorfano,Oxilorphane,Bristol laboratories BC 2605,levo-BC-2605

Cat.No: T60074

Synonym: 4-(Cyclopropylamino)-3-nitrobenzoic acid

Target: GPR

Urotensin II, mouse acetate (9047-55-6 free base)

Cat.No: TP2165

Synonym: Urotensin II, mouse acetate

Target: GPR

Urotensin II (114-124), human acetate

Cat.No: TP1737L

Synonym: Urotensin II (114-124), human acetate(251293-28-4 free base)

Target: GPR

Apelin-12 acetate

Cat.No: T39823L

Synonym: Apelin-12 acetate (229961-08-4 Free base)

Target: Apelin receptor, p38 MAPK, JNK

BigLEN (mouse) acetate

Cat.No: TP2073L

Synonym: BigLEN (mouse) acetate (501036-69-7 Free base)

Target: GPR

Cat.No: T5422

Synonym: CID-1375606,CID1375606

Target: Others

Cat.No: T60199

Target: GPR

BPK-29 hydrochloride

Cat.No: T13586L

Target: Others

Cat.No: T0755

Synonym: Carbaglu,N-Carbamylglutamate,N-Carbamyl-L-glutamic acid,氨甲酰谷氨酸,Carbamylglutamic acid,Carbamino-L-glutamic acid,Ureidoglutaric acid

Target: Others

Neuropeptide S (Rat) acetate

Cat.No: TP1982L

Target: Neuropeptide Y Receptor

Cat.No: T19700

Synonym: IBC293,1-异丙基-1H-1,2,3-苯并噻唑-5-羧酸,IBC-293

Target: GPR

Cat.No: T67694

Target: Parasite

Cat.No: T37587

Target: ROR

Cat. No.	Product Name	Target	Signaling Pathways
T3S1251	Neoruscogenin	ROR	Metabolism
	Neoruscogenin 是甾体 sapogenin 家族的成员，是一种可生物利用且具有高亲和力的核受体RORα (NR1F1)激动剂。
T2834	Nobiletin Hexamethoxyflavone,川陈皮素,川皮苷	Apoptosis; MMP; Reactive Oxygen Species; ROR; Autophagy	Apoptosis; Autophagy; Immunology/Inflammation; Metabolism; NF-κB; Proteases/Proteasome
	Nobiletin (Hexamethoxyflavone) 是一种来自柑橘皮的聚甲氧基黄酮，是RORs 激动剂，可改善记忆力丧失。它可降低分化的 C2C12 肌管中的ROS 水平，并具有抗炎，抗癌，抗血管生成，抗增殖，抗转移和诱导细胞凋亡作用。
T13502	3-Oxo-5β-cholanoic acid 3-氧代-5β-胆烷酸,Dehydrolithocholic acid	ROR	Metabolism
	3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid) 是胆汁酸的一种代谢产物。3-Oxo-5β-cholanoic acid 直接与关键转录因子RORγt(Kd=1.13 μM) 结合抑制TH17细胞分化。
TN6715	7-Ketocholesterol	Others	Others
	7-Ketocholesterol 是胆固醇的代谢物。
T9719	3-Hydroxyoctanoic Acid	GPR	Endocrinology/Hormones; GPCR/G Protein
	3-Hydroxyoctanoic Acid 是作为能量代谢中间体的羟基羧酸 (HCA) 之一。它是孤儿受体 GPR109B 的激动剂。
T14063	7α,25-Dihydroxycholesterol 7α,25-OHC	EBI2/GPR183; Endogenous Metabolite	GPCR/G Protein; Metabolism
	7α,25-Dihydroxycholesterol 是一种孤儿 GPCR 受体EBI2 (GPR183)的内源性配体和有效选择性激动剂。它对激活 EBI2 有很强的作用 (EC50=140 pM;Kd=450 pM)。它能够作为一种趋化因子，指导 B 细胞、T 细胞和树突状细胞的迁移。

天然产物

Cat.No: T3S1251

Target: ROR

Cat.No: T2834

Synonym: Hexamethoxyflavone,川陈皮素,川皮苷

Target: Apoptosis, MMP, Reactive Oxygen Species, ROR, Autophagy

3-Oxo-5β-cholanoic acid

Cat.No: T13502

Synonym: 3-氧代-5β-胆烷酸,Dehydrolithocholic acid

Target: ROR

7-Ketocholesterol

Cat.No: TN6715

Target: Others

3-Hydroxyoctanoic Acid

Cat.No: T9719

Target: GPR

7α,25-Dihydroxycholesterol

Cat.No: T14063

Synonym: 7α,25-OHC

Target: EBI2/GPR183, Endogenous Metabolite

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