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MedKoo Cat#: 526826 | Name: Reldesemtiv
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Description:

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

Reldesemtiv, also known as CK-107 and CK-2127107, is a fast skeletal troponin activator. Reldesemtiv improves exercise tolerance and increases performance in a rat model of heart failure. Reldesemtiv may offer clinical benefit and support evaluation in larger spinal muscular atrophy (SMA) patient populations. Reldesemtiv is a second-generation fast skeletal muscle troponin activator (FSTA) that increases force production at submaximal stimulation frequencies.

Chemical Structure

Reldesemtiv
Reldesemtiv
CAS#1345410-31-2 (free base)

Theoretical Analysis

MedKoo Cat#: 526826

Name: Reldesemtiv

CAS#: 1345410-31-2 (free base)

Chemical Formula: C19H18F2N6O

Exact Mass: 384.1510

Molecular Weight: 384.39

Elemental Analysis: C, 59.37; H, 4.72; F, 9.88; N, 21.86; O, 4.16

Price and Availability

Size Price Availability Quantity
5mg USD 850.00 2 Weeks
10mg USD 1,550.00 2 Weeks
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Related CAS #
Reldesemtiv HCl
Synonym
CK-2127107; CK2127107; CK 2127107; CK-107; CK 107; CK107; Reldesemtiv
IUPAC/Chemical Name
1-[2-({[trans-3-Fluoro-1-(3-fluoropyridin-2-yl)cyclobutyl]methyl}amino)pyrimidin-5-yl]-1H-pyrrole-3- carboxamide
InChi Key
MQXWPWOCXGARRK-HJGJAMNPSA-N
InChi Code
InChI=1S/C19H18F2N6O/c20-13-6-19(7-13,16-15(21)2-1-4-23-16)11-26-18-24-8-14(9-25-18)27-5-3-12(10-27)17(22)28/h1-5,8-10,13H,6-7,11H2,(H2,22,28)(H,24,25,26)/t13-,19-
SMILES Code
O=C(C1=CN(C2=CN=C(NC[C@]3(C4=NC=CC=C4F)C[C@H](F)C3)N=C2)C=C1)N
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
>2 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
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Reldesemtiv is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM.
In vitro activity:
While not specific to reldesemtiv, this article review both repurposed drugs and small-molecule compounds discovered, one being reldesemtiv, following medicinal chemistry optimization for the potential treatment of spinal muscular atrophy. Reference: J Med Chem. 2016 Nov 23;59(22):10067-10083. https://pubmed.ncbi.nlm.nih.gov/27490705/
In vivo activity:
Reldesemtiv substantially increases exercise performance in rats exhibiting heart failure-mediated skeletal myopathy. These results suggest that the modulation of skeletal muscle function by a fast skeletal troponin activator may be a useful therapeutic in heart failure-associated exercise intolerance. Reference: J Pharmacol Exp Ther. 2015 Apr;353(1):159-68. https://pubmed.ncbi.nlm.nih.gov/25678535/
Solvent mg/mL mM
Solubility
DMSO 18.6 30.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 384.39 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.

Recalculate based on batch purity %
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
Formulation protocol:
1. Calder AN, Androphy EJ, Hodgetts KJ. Small Molecules in Development for the Treatment of Spinal Muscular Atrophy. J Med Chem. 2016 Nov 23;59(22):10067-10083. doi: 10.1021/acs.jmedchem.6b00670. Epub 2016 Aug 16. PMID: 27490705; PMCID: PMC5744254. 2. Shefner JM, Andrews JA, Genge A, Jackson C, Lechtzin N, Miller TM, Cockroft BM, Meng L, Wei J, Wolff AA, Malik FI, Bodkin C, Brooks BR, Caress J, Dionne A, Fee D, Goutman SA, Goyal NA, Hardiman O, Hayat G, Heiman-Patterson T, Heitzman D, Henderson RD, Johnston W, Karam C, Kiernan MC, Kolb SJ, Korngut L, Ladha S, Matte G, Mora JS, Needham M, Oskarsson B, Pattee GL, Pioro EP, Pulley M, Quan D, Rezania K, Schellenberg KL, Schultz D, Shoesmith C, Simmons Z, Statland J, Sultan S, Swenson A, Berg LHVD, Vu T, Vucic S, Weiss M, Whyte-Rayson A, Wymer J, Zinman L, Rudnicki SA. A Phase 2, Double-Blind, Randomized, Dose-Ranging Trial Of Reldesemtiv In Patients With ALS. Amyotroph Lateral Scler Frontotemporal Degener. 2021 May;22(3-4):287-299. doi: 10.1080/21678421.2020.1822410. Epub 2020 Sep 24. PMID: 32969758; PMCID: PMC8117790. 3. Hwee DT, Kennedy AR, Hartman JJ, Ryans J, Durham N, Malik FI, Jasper JR. The small-molecule fast skeletal troponin activator, CK-2127107, improves exercise tolerance in a rat model of heart failure. J Pharmacol Exp Ther. 2015 Apr;353(1):159-68. doi: 10.1124/jpet.114.222224. Epub 2015 Feb 12. PMID: 25678535.
In vitro protocol:
1. Calder AN, Androphy EJ, Hodgetts KJ. Small Molecules in Development for the Treatment of Spinal Muscular Atrophy. J Med Chem. 2016 Nov 23;59(22):10067-10083. doi: 10.1021/acs.jmedchem.6b00670. Epub 2016 Aug 16. PMID: 27490705; PMCID: PMC5744254.
In vivo protocol:
1. Shefner JM, Andrews JA, Genge A, Jackson C, Lechtzin N, Miller TM, Cockroft BM, Meng L, Wei J, Wolff AA, Malik FI, Bodkin C, Brooks BR, Caress J, Dionne A, Fee D, Goutman SA, Goyal NA, Hardiman O, Hayat G, Heiman-Patterson T, Heitzman D, Henderson RD, Johnston W, Karam C, Kiernan MC, Kolb SJ, Korngut L, Ladha S, Matte G, Mora JS, Needham M, Oskarsson B, Pattee GL, Pioro EP, Pulley M, Quan D, Rezania K, Schellenberg KL, Schultz D, Shoesmith C, Simmons Z, Statland J, Sultan S, Swenson A, Berg LHVD, Vu T, Vucic S, Weiss M, Whyte-Rayson A, Wymer J, Zinman L, Rudnicki SA. A Phase 2, Double-Blind, Randomized, Dose-Ranging Trial Of Reldesemtiv In Patients With ALS. Amyotroph Lateral Scler Frontotemporal Degener. 2021 May;22(3-4):287-299. doi: 10.1080/21678421.2020.1822410. Epub 2020 Sep 24. PMID: 32969758; PMCID: PMC8117790. 2. Hwee DT, Kennedy AR, Hartman JJ, Ryans J, Durham N, Malik FI, Jasper JR. The small-molecule fast skeletal troponin activator, CK-2127107, improves exercise tolerance in a rat model of heart failure. J Pharmacol Exp Ther. 2015 Apr;353(1):159-68. doi: 10.1124/jpet.114.222224. Epub 2015 Feb 12. PMID: 25678535.
1: Rudnicki SA, Andrews JA, Duong T, Cockroft BM, Malik FI, Meng L, Wei J, Wolff AA, Genge A, Johnson NE, Tesi-Rocha C, Connolly AM, Darras BT, Felice K, Finkel RS, Shieh PB, Mah JK, Statland J, Campbell C, Habib AA, Kuntz NL, Oskoui M, Day JW. Reldesemtiv in Patients with Spinal Muscular Atrophy: a Phase 2 Hypothesis- Generating Study. Neurotherapeutics. 2021 Apr;18(2):1127-1136. doi: 10.1007/s13311-020-01004-3. Epub 2021 Feb 23. Erratum in: Neurotherapeutics. 2021 Jul;18(3):2130. doi: 10.1007/s13311-021-01120-8. PMID: 33624184; PMCID: PMC8423982. 2: Shefner JM, Andrews JA, Genge A, Jackson C, Lechtzin N, Miller TM, Cockroft BM, Meng L, Wei J, Wolff AA, Malik FI, Bodkin C, Brooks BR, Caress J, Dionne A, Fee D, Goutman SA, Goyal NA, Hardiman O, Hayat G, Heiman-Patterson T, Heitzman D, Henderson RD, Johnston W, Karam C, Kiernan MC, Kolb SJ, Korngut L, Ladha S, Matte G, Mora JS, Needham M, Oskarsson B, Pattee GL, Pioro EP, Pulley M, Quan D, Rezania K, Schellenberg KL, Schultz D, Shoesmith C, Simmons Z, Statland J, Sultan S, Swenson A, Berg LHVD, Vu T, Vucic S, Weiss M, Whyte-Rayson A, Wymer J, Zinman L, Rudnicki SA. A Phase 2, Double-Blind, Randomized, Dose-Ranging Trial Of Reldesemtiv In Patients With ALS. Amyotroph Lateral Scler Frontotemporal Degener. 2021 May;22(3-4):287-299. doi: 10.1080/21678421.2020.1822410. Epub 2020 Sep 24. PMID: 32969758; PMCID: PMC8117790. 3: Jiang J, Wang Y, Deng M. New developments and opportunities in drugs being trialed for amyotrophic lateral sclerosis from 2020 to 2022. Front Pharmacol. 2022 Nov 28;13:1054006. doi: 10.3389/fphar.2022.1054006. PMID: 36518658; PMCID: PMC9742490. 4: Collibee SE, Bergnes G, Chuang C, Ashcraft L, Gardina J, Garard M, Jamison CR, Lu K, Lu PP, Muci A, Romero A, Valkevich E, Wang W, Warrington J, Yao B, Durham N, Hartman J, Marquez A, Hinken A, Schaletzky J, Xu D, Hwee DT, Morgans D, Malik FI, Morgan BP. Discovery of Reldesemtiv, a Fast Skeletal Muscle Troponin Activator for the Treatment of Impaired Muscle Function. J Med Chem. 2021 Oct 28;64(20):14930-14941. doi: 10.1021/acs.jmedchem.1c01067. Epub 2021 Oct 12. PMID: 34636234. 5: Rudnicki SA, Andrews JA, Duong T, Cockroft BM, Malik FI, Meng L, Wei J, Wolff AA, Genge A, Johnson NE, Tesi-Rocha C, Connolly AM, Darras BT, Felice K, Finkel RS, Shieh PB, Mah JK, Statland J, Campbell C, Habib AA, Kuntz NL, Oskoui M, Day JW. Correction to: Reldesemtiv in Patients with Spinal Muscular Atrophy: a Phase 2 Hypothesis-Generating Study. Neurotherapeutics. 2021 Jul;18(3):2130. doi: 10.1007/s13311-021-01120-8. Erratum for: Neurotherapeutics. 2021 Apr;18(2):1127-1136. doi: 10.1007/s13311-020-01004-3. PMID: 34731415; PMCID: PMC8609058. 6: Shefner JM, Al-Chalabi A, Andrews JA, Chio A, De Carvalho M, Cockroft BM, Corcia P, Couratier P, Cudkowicz ME, Genge A, Hardiman O, Heiman-Patterson T, Henderson RD, Ingre C, Jackson CE, Johnston W, Lechtzin N, Ludolph A, Maragakis NJ, Miller TM, Mora Pardina JS, Petri S, Simmons Z, Van Den Berg LH, Zinman L, Kupfer S, Malik FI, Meng L, Simkins TJ, Wei J, Wolff AA, Rudnicki SA. COURAGE- ALS: a randomized, double-blind phase 3 study designed to improve participant experience and increase the probability of success. Amyotroph Lateral Scler Frontotemporal Degener. 2023 Aug;24(5-6):523-534. doi: 10.1080/21678421.2023.2216223. Epub 2023 May 30. PMID: 37254449. 7: Rudnicki SA, Andrews JA, Genge A, Jackson C, Lechtzin N, Miller TM, Cockroft BM, Malik FI, Meng L, Wei J, Wolff AA, Shefner JM; FORTITUDE-ALS STUDY GROUP. Prescription and acceptance of durable medical equipment in FORTITUDE-ALS, a study of reldesemtiv in ALS: post hoc analyses of a randomized, double- blind, placebo-controlled clinical trial. Amyotroph Lateral Scler Frontotemporal Degener. 2022 May;23(3-4):263-270. doi: 10.1080/21678421.2021.1946083. Epub 2021 Jul 5. PMID: 34218726. 8: Issahaku AR, Ibrahim MAA, Mukelabai N, Soliman MES. Intermolecular And Dynamic Investigation of The Mechanism of Action of Reldesemtiv on Fast Skeletal Muscle Troponin Complex Toward the Treatment of Impaired Muscle Function. Protein J. 2023 Aug;42(4):263-275. doi: 10.1007/s10930-023-10091-y. Epub 2023 Mar 23. PMID: 36959428; PMCID: PMC10352438. 9: Gebrehiwet P, Meng L, Rudnicki SA, Sarocco P, Wei J, Wolff AA, Butzner M, Chiò A, Andrews JA, Genge A, Hughes DA, Jackson CE, Lechtzin N, Miller TM, Shefner JM. Health utilities and quality-adjusted life years for patients with amyotrophic lateral sclerosis receiving reldesemtiv or placebo in FORTITUDE-ALS. J Med Econ. 2023 Jan-Dec;26(1):488-493. doi: 10.1080/13696998.2023.2192588. PMID: 36930042. 10: Gebrehiwet P, Meng L, Rudnicki SA, Sarocco P, Wei J, Wolff AA, Chiò A, Andrews JA, Genge A, Jackson CE, Lechtzin N, Miller TM, Shefner JM. MiToS and King's staging as clinical outcome measures in ALS: a retrospective analysis of the FORTITUDE-ALS trial. Amyotroph Lateral Scler Frontotemporal Degener. 2023 May;24(3-4):304-310. doi: 10.1080/21678421.2022.2154678. Epub 2022 Dec 12. PMID: 36503310. 11: Shefner JM, Jacobsen B, Kupfer S, Malik FI, Meng L, Wei J, Wolff AA, Rudnicki SA. Relationship between quantitative strength and functional outcomes in the phase 2 FORTITUDE-ALS trial. Amyotroph Lateral Scler Frontotemporal Degener. 2024 Feb;25(1-2):162-169. doi: 10.1080/21678421.2023.2252468. Epub 2023 Aug 29. PMID: 37641579.