Dersimelagon | CAS#1835256-48-8 | melanocortin receptor agonist

MedKoo Cat#: 563458 | Name: Dersimelagon

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Dersimelagon, also known as MT-7117 and WHO 10832, is a novel, orally-administered, small molecule, 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. Dersimelagon significantly boosted sunlight tolerance in patients with erythropoietic protoporphyria in a multicenter, phase 2, randomized trial.

Chemical Structure

Dersimelagon

CAS#1835256-48-8 (free base)

Theoretical Analysis

MedKoo Cat#: 563458

Name: Dersimelagon

CAS#: 1835256-48-8 (free base)

Chemical Formula: C36H45F4N3O5

Exact Mass: 675.3295

Molecular Weight: 675.77

Elemental Analysis: C, 63.99; H, 6.71; F, 11.25; N, 6.22; O, 11.84

Price and Availability

Size	Price	Availability
10mg	USD 350.00	2 Weeks
25mg	USD 550.00	2 Weeks
50mg	USD 950.00	2 Weeks
100mg	USD 1,650.00	2 Weeks
1g	USD 5,850.00	2 Weeks

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Related CAS #

2490660-87-0 (phosphate) 1835256-48-8 (free base)

Synonym

Dersimelagon; MT-7117; MT7117; MT7117; WHO 10832; WHO-10832; WHO10832;

IUPAC/Chemical Name

1-(2-((3S,4R)-1-((3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl)pyrrolidine-3-carbonyl)-4-(methoxymethyl)pyrrolidin-3-yl)-5-(trifluoromethyl)phenyl)piperidine-4-carboxylic acid

InChi Key

MUNWOYRHJPWQNE-GMFUQMJFSA-N

InChi Code

InChI=1S/C36H45F4N3O5/c1-47-21-25-18-42(19-30(25)29-12-9-26(36(38,39)40)17-32(29)41-15-13-24(14-16-41)33(44)45)34(46)35(37)22-43(27-5-3-4-6-27)20-31(35)23-7-10-28(48-2)11-8-23/h7-12,17,24-25,27,30-31H,3-6,13-16,18-22H2,1-2H3,(H,44,45)/t25-,30+,31+,35+/m1/s1

SMILES Code

O=C(C1CCN(C2=CC(C(F)(F)F)=CC=C2[C@H]3CN(C([C@]4(F)CN(C5CCCC5)C[C@H]4C6=CC=C(OC)C=C6)=O)C[C@@H]3COC)CC1)O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.03.00

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 675.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Balwani M, Bonkovsky HL, Levy C, Anderson KE, Bissell DM, Parker C, Takahashi F, Desnick RJ, Belongie K; Endeavor Investigators. Dersimelagon in Erythropoietic Protoporphyrias. N Engl J Med. 2023 Apr 13;388(15):1376-1385. doi: 10.1056/NEJMoa2208754. PMID: 37043653. 2: Madigan KE, Rudnick SR, Agnew MA, Urooj N, Bonkovsky HL. Illuminating Dersimelagon: A Novel Agent in the Treatment of Erythropoietic Protoporphyria and X-Linked Protoporphyria. Pharmaceuticals (Basel). 2023 Dec 25;17(1):31. doi: 10.3390/ph17010031. PMID: 38256864; PMCID: PMC10819203. 3: Balwani M, Desnick RJ, Belongie K. Dersimelagon in Erythropoietic Protoporphyrias. Reply. N Engl J Med. 2023 Jun 29;388(26):2492-2493. doi: 10.1056/NEJMc2305601. PMID: 37379151. 4: Barman-Aksözen J, Langendonk JG. Dersimelagon in Erythropoietic Protoporphyrias. N Engl J Med. 2023 Jun 29;388(26):2492. doi: 10.1056/NEJMc2305601. PMID: 37379150. 5: Granata F, Dechant C, Falchetto R. Dersimelagon in Erythropoietic Protoporphyrias. N Engl J Med. 2023 Jun 29;388(26):2491-2492. doi: 10.1056/NEJMc2305601. PMID: 37379149. 6: Kondo M, Suzuki T, Kawano Y, Kojima S, Miyashiro M, Matsumoto A, Kania G, Błyszczuk P, Ross RL, Mulipa P, Del Galdo F, Zhang Y, Distler JHW. Dersimelagon, a novel oral melanocortin 1 receptor agonist, demonstrates disease-modifying effects in preclinical models of systemic sclerosis. Arthritis Res Ther. 2022 Sep 1;24(1):210. doi: 10.1186/s13075-022-02899-3. PMID: 36050717; PMCID: PMC9434962. 7: Ogasawara A, Ogawa K, Ide R, Ikenaga Y, Fukunaga C, Nakayama S, Tsuda M. Results from a first-in-human study of dersimelagon, an investigational oral selective MC1R agonist. Eur J Clin Pharmacol. 2023 Jun;79(6):801-813. doi: 10.1007/s00228-023-03476-6. Epub 2023 Apr 15. PMID: 37060458; PMCID: PMC10229459. 8: Ogawa K, Ide R, Belongie K, Tsuda M, Kawanishi H, Teng R, Ogasawara A. The Oral Bioavailability and Effect of Various Gastric Conditions on the Pharmacokinetics of Dersimelagon in Healthy Adult Volunteers. Clin Pharmacol Drug Dev. 2023 May;12(5):493-501. doi: 10.1002/cpdd.1235. Epub 2023 Feb 25. PMID: 36840969. 9: Tsuda M, Ogawa K, Endou T, Goto T, Ogasawara Y, Ogasawara A. Absorption, metabolism, and excretion of [¹⁴ C]dersimelagon, an investigational oral selective melanocortin 1 receptor agonist, in preclinical species and healthy volunteers. Pharmacol Res Perspect. 2023 Jun;11(3):e01084. doi: 10.1002/prp2.1084. PMID: 37078227; PMCID: PMC10116397. 10: Suzuki T, Kawano Y, Matsumoto A, Kondo M, Funayama K, Tanemura S, Miyashiro M, Nishi A, Yamada K, Tsuda M, Sato A, Morokuma K, Yamamoto Y. Melanogenic effect of dersimelagon (MT-7117), a novel oral melanocortin 1 receptor agonist. Skin Health Dis. 2021 Nov 29;2(1):e78. doi: 10.1002/ski2.78. PMID: 35665216; PMCID: PMC9060023.