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).
- Cat.No. 产品名称 Information
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GC66383
ACTH (11-24) (acetate)
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GC64525
Fenoprofen
An NSAID
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GC64427
MK-0493
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GC63770
HS024 TFA
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GC63756
PG106 TFA
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GC63724
HS014 TFA
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GC61462
γ-1-Melanocyte Stimulating Hormone (MSH), amide
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GC50303
MSG 606
MSG-606 has potent antagonist activity and receptor selectivity for the human melanocortin 1 receptor (hMC1R) (IC50 = 17 nM) .
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GC38107
SNT-207858 free base
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GC38007
β-Melanocyte Stimulating Hormone (MSH), human TFA
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GC37629
Setmelanotide TFA
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GC36756
Nonapeptide-1 acetate salt
An MC1R antagonist
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GC36727
Neuropeptide EI, rat
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GC35255
Adrenocorticotropic Hormone (ACTH) (1-39), rat TFA
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GC35254
Adrenocorticotropic Hormone (ACTH) (1-39), rat
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GC35244
ACTH (1-17) TFA
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GC34231
γ-1-Melanocyte Stimulating Hormone (MSH), amide
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GC34002
Bremelanotide Acetate (PT-141 Acetate)
A cyclic peptide agonist of MC4R
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GC33693
β-Melanocyte Stimulating Hormone (MSH), human (Beta-MSH (1-22) (human))
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GC32420
PF-00446687
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GC31954
ACTH 11-24 (Adrenocorticotropic Hormone (11-24))
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GC31629
MC-4R Agonist 1
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GC31600
SNT-207707
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GC31560
SNT-207858
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GC31109
ACTH 1-17 (α1-17-ACTH)
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GC30372
Setmelanotide (RM-493)
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.
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GC30194
JNJ-10229570
JNJ-10229570 (UNII-N9IX402L35) is a potent MC1R and MC5R antagonist.
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GC18458
Terrein
A fungal metabolite with diverse biological activities
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GC13798
ML 00253764 hydrochloride
A MC4R antagonist
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GC17626
PG 931
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。
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GC12163
PG 106
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。
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GC13806
Lys-γ3-MSH
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。
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GC12239
ACTH (1-39)
A MC2R agonist
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GC14127
MCL 0020
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。
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GC10701
JKC 363
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。
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GC17002
γ1-MSH
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。
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GC13565
SHU 9119
An MC1R agonist and MC4R antagonist
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GC13068
[Nle4,D-Phe7]-α-MSH
A synthetic analog of α-MSH
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GC10747
HS 024
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。
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GC12840
HS 014
HS 014 是一种有效的选择性黑皮质素 4 (MC4) 受体拮抗剂,对人 MC4、MC1、MC3 和 MC5 受体的 Kis 分别为 3.16、108、54.4 和 694 nM。
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GC10947
[D-Trp8]-γ-MSH
An MC3R agonist
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GC16069
THIQ
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。
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GC14374
α-MSH
α-MSH (α-Melanocyte-Stimulating Hormone) 是一种内源性神经肽,是一种具有抗炎和解热活性的内源性黑皮质素受体 4 (MC4R) 激动剂。
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GC16276
Melanotan II
A melanocortin receptor agonist