SRT3190 (SRT-3190) is a potent and selective antagonist of CXCR2 (C-X-C chemokine receptor type 2) and an activator of SIRT1 with anti-Inflammatory and immunomodulatory activity. SRT3190 may find application in the study of diseases mediated by chemokines. Integral membrane proteins known as CXCRs (CXC chemokine receptors) bind and react specifically to cytokines within the CXC chemokine family. Given that they span the cell membrane seven times, they are referred to as seven transmembrane (7-TM) proteins, and they constitute one subfamily of the large family of G protein-linked chemokine receptors. Currently, CXCR1 through CXCR7 are the seven CXC chemokine receptors that are known to exist in mammals. Closely related receptors CXCR1 and CXCR2 are able to identify CXC chemokines with an E-L-R amino acid motif right next to their CXC motif.
Physicochemical Properties
| Molecular Formula | C18H23F2N5O4S2 | |
| Molecular Weight | 475.53 | |
| Exact Mass | 475.116 | |
| Elemental Analysis | C, 45.46; H, 4.88; F, 7.99; N, 14.73; O, 13.46; S, 13.48 | |
| CAS # | 1204707-73-2 | |
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| PubChem CID | 59149652 | |
| Appearance | White to off-white solid powder | |
| LogP | 2.727 | |
| Hydrogen Bond Donor Count | 4 | |
| Hydrogen Bond Acceptor Count | 12 | |
| Rotatable Bond Count | 10 | |
| Heavy Atom Count | 31 | |
| Complexity | 670 | |
| Defined Atom Stereocenter Count | 2 | |
| SMILES | OC[C@@H]([C@@H](NC1=CC(NS(N2CCC2)(=O)=O)=NC(SCC3=C(C(F)=CC=C3)F)=N1)C)O |
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| InChi Key | QVKPEMXUBULFBM-FZMZJTMJSA-N | |
| InChi Code | InChI=1S/C18H23F2N5O4S2/c1-11(14(27)9-26)21-15-8-16(24-31(28,29)25-6-3-7-25)23-18(22-15)30-10-12-4-2-5-13(19)17(12)20/h2,4-5,8,11,14,26-27H,3,6-7,9-10H2,1H3,(H2,21,22,23,24)/t11-,14-/m0/s1 | |
| Chemical Name | N-[2-[(2,3-difluorophenyl)methylsulfanyl]-6-[[(2S,3R)-3,4-dihydroxybutan-2-yl]amino]pyrimidin-4-yl]azetidine-1-sulfonamide | |
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| HS Tariff Code | 2934.99.9001 | |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | CXCR2 |
| ln Vitro | SRT3190 (Reference Example 2) an antagonist of CXCR2, is utilized in the research of chemokine mediated diseases[1]. |
| References |
[1]. Pyrimidyl sulfonaminde derivative and its use for the treatment of chemokine mediated diseases. WO2010007427A1. |
Solubility Data
| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.26 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 (5.26 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1029 mL | 10.5146 mL | 21.0292 mL | |
| 5 mM | 0.4206 mL | 2.1029 mL | 4.2058 mL | |
| 10 mM | 0.2103 mL | 1.0515 mL | 2.1029 mL |