Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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Other Sizes |
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Difelikefalin (MR-13A9; CR-845; MR-13A-9; trade name Korsuva) is a novel, peripherally specific, and potent kappa opioid receptor agonist approved in 2021 as an analgesic opiod peptide for the treatment of moderate-to-severe itching. In August 2021, difelikefalin received FDA approval for medical use in the US.
Targets |
kappa opioid receptor (KOR)
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ln Vitro |
Difelikefalin (CR-845; FE-202845) does not penetrate the blood-brain barrier. Difelikefalin does not bind to any receptors other than KORs, including mu opioid receptors[1].
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References |
Molecular Formula |
C36H53N7O6
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Molecular Weight |
679.86
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Exact Mass |
679.41
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Elemental Analysis |
C, 63.60; H, 7.86; N, 14.42; O, 14.12
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CAS # |
1024828-77-0
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Related CAS # |
413256-25-2 (1HCl); 1024829-44-4 (acetate); 1024828-77-0; 2711717-77-8 (3HCl); 2742623-88-5 (TFA)
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Appearance |
Solid powder
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SMILES |
CC(C)C[C@H](C(=O)N[C@H](CCCCN)C(=O)N1CCC(CC1)(C(=O)O)N)NC(=O)[C@@H](CC2=CC=CC=C2)NC(=O)[C@@H](CC3=CC=CC=C3)N
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InChi Key |
FWMNVWWHGCHHJJ-SKKKGAJSSA-N
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InChi Code |
InChI=1S/C36H53N7O6/c1-24(2)21-29(32(45)40-28(15-9-10-18-37)34(47)43-19-16-36(39,17-20-43)35(48)49)42-33(46)30(23-26-13-7-4-8-14-26)41-31(44)27(38)22-25-11-5-3-6-12-25/h3-8,11-14,24,27-30H,9-10,15-23,37-39H2,1-2H3,(H,40,45)(H,41,44)(H,42,46)(H,48,49)/t27-,28-,29-,30-/m1/s1
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Chemical Name |
4-amino-1-[(2R)-6-amino-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid
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Synonyms |
MR-13A9; CR-845; MR-13A-9; MR13A9; CR845; MR13A-9; trade name Korsuva
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~100 mg/mL (~147.1 mM)
H2O: ≥ 100 mg/mL (~147.1 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4709 mL | 7.3545 mL | 14.7089 mL | |
5 mM | 0.2942 mL | 1.4709 mL | 2.9418 mL | |
10 mM | 0.1471 mL | 0.7354 mL | 1.4709 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05342623 | Recruiting | Drug: Difelikefalin 1 mg Oral Tablet Drug: Placebo Oral Tablet |
Chronic Kidney Diseases Pruritus |
Cara Therapeutics, Inc. | May 17, 2022 | Phase 3 |
NCT05356403 | Recruiting | Drug: Difelikefalin 1 mg Oral Tablet Drug: Placebo Oral Tablet |
Chronic Kidney Diseases Pruritus |
Cara Therapeutics, Inc. | August 26, 2022 | Phase 3 |
NCT05885737 | Recruiting | Drug: Difelikefalin Injection Drug: Placebo Injection |
Uremic Pruritus | Vifor Fresenius Medical Care Renal Pharma |
May 30, 2023 | Phase 3 |
NCT05387707 | Recruiting | Drug: difelikefalin 0.25 mg Drug: difelikefalin 0.5 mg |
Pruritus Atopic Dermatitis |
Cara Therapeutics, Inc. | August 16, 2022 | Phase 3 |
NCT05978063 | Recruiting | Drug: difelikefalin 2.0 mg tablets Drug: Placebo tablets |
Pruritus Notalgia Paresthetica |
Cara Therapeutics, Inc. | August 1, 2023 | Phase 2 Phase 3 |
Change from baseline at week 8 in the weekly mean of the daily 24-hour Worst Itching Intensity Numerical Rating Scale (WI-NRS) scores for difelikefalin versus placebo. Kidney Int Rep . 2020 Jan 28;5(5):600-610. td> |
Changes from baseline at week 8 in quality-of-life (QoL) measures for difelikefalin versus placebo as per Skindex-10 total score (left) and 5-D itch total score (right). Kidney Int Rep . 2020 Jan 28;5(5):600-610. td> |
Percentage of patients per Patient Global Impression of Change categories on 8 weeks of exposure to all difelikefalin combined or placebo. Kidney Int Rep . 2020 Jan 28;5(5):600-610. td> |