Melanocortin (MC) Receptors
Melanocortin (MC) Receptors(黑皮质素 (MC) 受体)
Melanocortin receptors (MCRs) comprise a family of five, class A, G protein-coupled receptors designated MC1R-MC5R with diverse physiological roles. MCRs are found in chordates and are regarded as having evolved from a single ancestral receptor, possibly corresponding most closely to MC4R. Signaling by MCRs has primarily been observed as occurring through the stimulatory α unit Gs which activates adenylyl cyclase to produce cAMP.
The central nervous melanocortin system is involved in energy homeostasis, regulating food intake and energy expenditure. The brain melanocortin system is defined as the primary neurons that express neuropeptide ligands, and secondary neurons expressing the predominant neural melanocortin receptors (MC3R, MC4R). Mutations in the gene encoding melanocortin receptor agonists, or the genes encoding MC3R or MC4R cause obesity. The other members of the melanocortin receptor family are primarily expressed in the periphery, and are involved in regulating pigmentation (MC1R), adrenal gland function (MC2R), immune function (MC1R/MC3R), and sebaceous gland activity (MC5R).
Melanocortin (MC) Receptors 相关产品(54)
- GC12239Adrenocorticotropic Hormone (ACTH) (1-39)CAS: 12279-41-3纯度: >98.00%
Adrenocorticotropic Hormone (ACTH) (1-39)是一种由垂体前叶产生的有效的黑皮质素2受体(MC2R)激动剂。
- GC30194JNJ-10229570CAS: 524923-88-4纯度: >98.00%
JNJ-10229570 (UNII-N9IX402L35) is a potent MC1R and MC5R antagonist.
- GC30372Setmelanotide (RM-493)CAS: 920014-72-8
Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM.
- GC31109ACTH 1-17 (α1-17-ACTH)CAS: 7266-47-9
ACTH 1-17 (α1-17-ACTH) 是一种促肾上腺皮质激素类似物,是一种有效的人黑皮质素 1 (MC1) 受体激动剂,Ki 为 0.21 nM。
- GC31560SNT-207858CAS: 1104080-42-3
SNT-207858是一种选择性,有口服活性的黑皮质素(melanocortinMC-4)受体拮抗剂,选择性分别是MC-3和MC-5的170和40倍。SNT-207858对MC-4受体的IC50值为8nM(结合)and5nM(功能)。
- GC31600SNT-207707CAS: 1064662-40-3纯度: >99.00%
SNT-207707是一种有效,选择性,有口服活性的黑素皮质素受体(melanocortinMC-4)拮抗剂,IC50值为8nM(结合)和5nM(功能)。
- GC31629MC-4R Agonist 1CAS: 455957-28-5
MC-4RAgonist1是一种黑素皮质素受体4(humanmelanocortin-4receptor)的激动剂,可用于肥胖、糖尿病及性功能紊乱等疾病的研究。
- GC31954ACTH 11-24 (Adrenocorticotropic Hormone (11-24))CAS: 4237-93-8
ACTH 11-24 (Adrenocorticotropic Hormone (11-24)) 是一种促肾上腺皮质激素 (ACTH) 受体拮抗剂。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC10701 | JKC 363 | 436083-30-6 | - | |
JKC 363 是一种选择性黑皮质素 MC4 受体拮抗剂,对 MC4 受体的亲和力 (IC50\u003d0.5 nM) 是对 MC3 受体 (44.9 nM) 的 90 倍。 | ||||
| GC10747 | HS 024 | 212370-59-7 | - | |
HS 024 是一种选择性 MC4 受体拮抗剂,对 MC4、MC5、MC3 和 MC1 的 Kis 分别为 0.29、3.29、5.45 和 18.6 nM。 | ||||
| GC10947 | [D-Trp8]-γ-MSH | 321351-81-9 | - | |
An MC3R agonist | ||||
| GC12163 | PG 106 | 944111-22-2 | - | |
PG 106 是一种有效的选择性人黑皮质素 3 (hMC3) 受体拮抗剂 (IC50\u003d210 nM),对 hMC4 受体 (EC50\u003d9900 nM) 和 hMC5 受体没有活性。 | ||||
| GC12239 | Adrenocorticotropic Hormone (ACTH) (1-39) | 12279-41-3 | >98.00% | |
Adrenocorticotropic Hormone (ACTH) (1-39)是一种由垂体前叶产生的有效的黑皮质素2受体(MC2R)激动剂。 | ||||
| GC12840 | HS 014 | 207678-81-7 | - | |
HS 014是一种高效、选择性的黑皮质素MC4受体拮抗剂(K i =3.16nM)。 | ||||
| GC13068 | [Nle4,D-Phe7]-α-MSH | 75921-69-6 | >99.00% | |
A synthetic analog of α-MSH | ||||
| GC13565 | SHU 9119 | 168482-23-3 | >98.00% | |
An MC1R agonist and MC4R antagonist | ||||
| GC13798 | ML 00253764 hydrochloride | 1706524-94-8 | - | |
A MC4R antagonist | ||||
| GC13806 | Lys-γ3-MSH | 156159-18-1 | - | |
Lys-γ3-MSH 是一种源自阿片黑皮质素原 (POMC) 片段 C 末端的黑皮质素肽。 | ||||
| GC14127 | MCL 0020 | 475498-26-1 | - | |
MCL 0020 是一种有效的选择性黑皮质素 MC4 受体拮抗剂,IC50 为 11.63 nM。 | ||||
| GC14374 | α-MSH | 581-05-5 | >98.00% | |
α -黑色素细胞刺激激素(α-MSH)是一种具有免疫调节特性的神经肽,由原黑素皮质素(POMC)翻译后加工产生。 | ||||
| GC16069 | THIQ | 312637-48-2 | >98.00% | |
THIQ 是第一个选择性的黑皮质素 4 受体 (MC4R) 激动剂,对 hMC4R (IC50=1.2 nM, EC50=2.1 nM) 和 rMC4R (IC50=0.6 nM, EC50=2.9 nM) 具有高亲和力和效力。 | ||||
| GC16276 | Melanotan II | 121062-08-6 | >99.50% | |
A melanocortin receptor agonist | ||||
| GC17002 | γ1-MSH | 72629-65-3 | - | |
γ1-MSH 是一种黑皮质素 MC3 受体激动剂,对大鼠 MC3 受体的 Ki 值为 34 nM。 | ||||
| GC17626 | PG 931 | 667430-81-1 | - | |
PG 931 是 SHU 9119 的类似物,是一种有效的黑皮质素 4 (MC4) 受体 (IC50\u003d0.58 nM) 激动剂,比对 hMC3R (IC50\u003d55 nM) 或 hMC5R (IC50\u003d2.4 nM) 更具选择性。 | ||||
| GC18458 | Terrein | 582-46-7 | >98.00% | |
A fungal metabolite with diverse biological activities | ||||
| GC30194 | JNJ-10229570 | 524923-88-4 | >98.00% | |
JNJ-10229570 (UNII-N9IX402L35) is a potent MC1R and MC5R antagonist. | ||||
| GC30372 | Setmelanotide (RM-493) | 920014-72-8 | - | |
Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM. | ||||
| GC31109 | ACTH 1-17 (α1-17-ACTH) | 7266-47-9 | - | |
ACTH 1-17 (α1-17-ACTH) 是一种促肾上腺皮质激素类似物,是一种有效的人黑皮质素 1 (MC1) 受体激动剂,Ki 为 0.21 nM。 | ||||
| GC31560 | SNT-207858 | 1104080-42-3 | - | |
SNT-207858是一种选择性,有口服活性的黑皮质素(melanocortinMC-4)受体拮抗剂,选择性分别是MC-3和MC-5的170和40倍。SNT-207858对MC-4受体的IC50值为8nM(结合)and5nM(功能)。 | ||||
| GC31600 | SNT-207707 | 1064662-40-3 | >99.00% | |
SNT-207707是一种有效,选择性,有口服活性的黑素皮质素受体(melanocortinMC-4)拮抗剂,IC50值为8nM(结合)和5nM(功能)。 | ||||
| GC31629 | MC-4R Agonist 1 | 455957-28-5 | - | |
MC-4RAgonist1是一种黑素皮质素受体4(humanmelanocortin-4receptor)的激动剂,可用于肥胖、糖尿病及性功能紊乱等疾病的研究。 | ||||
| GC31954 | ACTH 11-24 (Adrenocorticotropic Hormone (11-24)) | 4237-93-8 | - | |
ACTH 11-24 (Adrenocorticotropic Hormone (11-24)) 是一种促肾上腺皮质激素 (ACTH) 受体拮抗剂。 | ||||
