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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T7589 |
Afamelanotide acetate
afamelanotide |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
Afamelanotide acetate 是一种合成的 α-黑素细胞刺激激素类似物和一流的黑皮质素-1 受体激动剂,用于治疗红细胞生成性原卟啉症。 | |||
TP1097 |
Melanotan I
美拉诺坦,美拉诺坦 I,[Nle4,D-Phe7]-α-MSH,Afamelanotide,MT-I |
Others | Others |
Melanotan I 是一种非特异性黑素皮质激素受体 (MCR) 激动剂, 是一种 α- 黑素细胞刺激激素 (α-MSH) 类似物,皮下注射可增加黑色素在皮肤中的含量。Melanotan I 可用于辅助美黑。Melanotan I 可用于预防阳光诱发皮肤癌,可用于研究黑色素瘤和男性勃起功能障碍。 | |||
T76670 |
hMC1R agonist 1
|
||
hMC1R agonist 1 是一种有效的选择性hMC1R 激动剂(EC50=3 nM),hMC1R agonist 1 对hMC1R 的选择性是hMC3R(b>EC50=902 nM),hMC4R(b>EC50=915 nM),和hMC5R(b>EC50=>1000 nM) 的 300 倍。hMC1R agonist 1 有研究和预防黑皮质素家族疾病的潜能。 | |||
T25310 |
Dersimelagon
MT-7117 |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
Dersimelagon (MT-7117) (MT-7117) 是一种具有口服活性的选择性黑皮质素 1 受体(MC1R) 激动剂,对人 (h)、食蟹猴 (cm)、小鼠 (m) 和大鼠 (r) MC1R 的 EC50 值分别为 8.16、3.91、1.14 和 0.251 nM。Dersimelagon 对 hMC1R 和 hMC4R 表现出良好的亲和力,Ki 值分别为 2.26 和 32.9 nM。Dersimelagon 可用于皮肤色素沉着的研究。 | |||
T5464 |
JNJ-10229570
JNJ10229570,UNII-N9IX402L35,JNJ 10229570 |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
JNJ-10229570 (UNII-N9IX402L35) 是肾上腺皮质受体 1 和肾上腺皮质受体 5 的拮抗剂,可抑制皮脂腺分化和皮质特异性脂质的产生,其抑制125I-NDP-α-MSH 和人类细胞中 MC1R 和 MC5R 结合的IC50值分别为 270 nM 和 200 nM。 | |||
TP1011L |
ACTH (1-17) acetate
|
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
ACTH (1-17) acetate 是一种有效的人黑皮质素 1 (MC1) 受体激动剂,具有高亲和力 (Ki = 0.21 nM)。 | |||
T70720 |
CD08108
|
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CD08108 is a MC1R agonist. | |||
TP2154 |
RO27-3225 TFA (274682-89-2 free base)
RO27-3225 TFA |
Others | Others |
RO27-3225 TFA is a potent and selective agonist of melanocortin 4 receptor (MC4R; EC50: 1 nM and 8 nM for MC4R and MC1R) with neuroprotective and anti-inflammatory effects. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. | |||
T69607 | Dersimelagon phosphate | ||
Dersimelagon phosphate is a selective melanocortin-1 receptor (MC1R) agonist that increases skin melanin without sun exposure and is being developed to increase light tolerance in EPP/XLP patients. | |||
T76072 |
CCZ01048
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CCZ01048 是一种 α-MSH 类似物,与黑素皮质素 1 受体(MC1R)具有很高的结合亲和力,Ki 值为 0.31 nM。CCZ01048 具有快速内化 B16F10 黑色素瘤细胞和高体内稳定性。CCZ01048 是恶性黑色素瘤 PET 显像的一个有前途的制剂。 | |||
T76072L |
CCZ01048 TFA
|
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CCZ01048 TFA 是一种 α-MSH 类似物,与黑素皮质素1受体(MC1R)具有很高的结合亲和力,Ki 值为 0.31 nM。CCZ01048 TFA 具有快速内化 B16F10 黑色素瘤细胞和高体内稳定性。CCZ01048 TFA 是恶性黑色素瘤 PET 显像的一个有前途的制剂。 | |||
T75715 |
Nonapeptide-1 acetate salt
|
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Nonapeptide-1 (Melanostatine-5) acetate salt,一种多肽类激素,是 MC1R 选择性拮抗剂 (Ki: 40 nM)。 Nonapeptide-1 acetate salt 是一种竞争性的α-MSH 拮抗剂,可有效抑制黑素细胞中 α-MSH 诱导的细胞内 cAMP 和黑素体扩散 (IC50分别为 2.5 nM 和 11 nM)。 Nonapeptide-1 acetate salt 抑制黑色素合成,可用于研究皮肤色素沉着和肾上腺类固醇生成的调节、皮肤癌。 | |||
T71559 | Melanotan II acetate | ||
Melanotan II acetate is an agonist of melanocortin receptor 1 (MC1R), MC3R, MC4R, and MC5R. It has been shown to improve recovery of sciatic nerve function after mechanical injury and increase cisplatin-induced decreases in sensory nerve conduction velocity. Melanotan II acetate increases oxygen consumption and protein levels of uncoupling protein 1 (UCP1) in brown adipose tissue homogenates and decreases food intake, body weight, and serum levels of leptin, glucose, insulin, and cholesterol. | |||
T12882L |
Setmelanotide Acetate(920014-72-8 free base)
RM-493 Acetate,IRC-022493 Acetate,BIM-22493 Acetate |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) 是黑皮质素 4 受体 (MC4R) 的选择性激动剂(人和大鼠 MC4R,EC50 分别为 0.27 nM 和 0.28 nM)。 | |||
T10568 |
BMS-470539 dihydrochloride
|
Others | Others |
BMS-470539 dihydrochloride is a highly potent and selective agonist of the melanocortin-1 receptor (MC-1R; IC50: 120 nM; EC50: 28 nM) with anti-inflammatory properties. It does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. | |||
T12882 |
Setmelanotide
BIM-22493,IRC-022493,RM-493 |
Melanocortin Receptor | GPCR/G Protein; Neuroscience |
Setmelanotide (BIM-22493) 是黑皮质素 4 受体 (MC4R) 的选择性激动剂(人和大鼠 MC4R,EC50 分别为 0.27 nM 和 0.28 nM)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TMA0003 | Trans-caffeic acid | cAMP; Tyrosinase | GPCR/G Protein; Proteases/Proteasome |
Trans-caffeic acid stearyl ester is posited to inhibit melanogenesis signaling while suppressing cAMP levels and, subsequently, MC1R, MITF, tyrosinase, TRP-2 and TRP-1 down-regulation, resulting in the suppression of tyrosinase activity, DOPA oxidase activity and melanin synthesis. |