| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
ATI-2341 TFA targets the C-X-C chemokine receptor type 4 (CXCR4), a G protein-coupled receptor that plays a key role in cell migration, retention of hematopoietic stem and progenitor cells in the bone marrow, and immune cell trafficking. It acts as an allosteric agonist and biased ligand, preferentially activating Galphai signaling over Galpha13 pathways, with downstream effects including inhibition of cAMP production and induction of calcium mobilization.
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| ln Vitro |
CXCR4[1]
In vitro, ATI-2341 induces CXCR4- and G protein-dependent signaling, receptor internalization, and chemotaxis in CXCR4-expressing cells. It is a potent agonist with an EC50 value of 194 +/- 16 nM and an intrinsic activity of 81 +/- 4% in endogenously CXCR4-expressing CCRF-CEM cells. It dose-dependently inhibits NKH477-induced cAMP accumulation in CXCR4-HEK cells but shows no effect in naïve HEK-293 parental cells. |
| ln Vivo |
In vivo, intraperitoneal injection of ATI-2341 in BALB/c mice results in a dose-dependent recruitment of PMNs into the peritoneum, with a maximal effect seen at 405 nmol/kg, although higher concentrations reduce recruitment (bell-shaped curve). Intravenous administration leads to a dose-dependent increase in PMNs in peripheral circulation, with maximal effect at 0.66 micromol/kg. No effect on lymphocyte mobilization is observed at any dose tested.
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| Enzyme Assay |
For ATI-2341 TFA, CXCR4 binding and allosteric modulation are assessed using radioligand binding assays and functional assays for G protein activation. The compound's binding characteristics are evaluated using membrane preparations from CXCR4-expressing cells. Additionally, BRET-based assays to measure dissociation of Galphai and Ggamma2 subunits are used to confirm Galphai-biased signaling. The EC50 for dissociation is 0.21 in this system.
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| Cell Assay |
For ATI-2341 TFA, CXCR4-expressing HEK-293 cells or CCRF-CEM cells (endogenously expressing CXCR4) are cultured and treated with varying concentrations of ATI-2341. Chemotaxis is assessed using Transwell plates, measuring cell migration toward the compound. cAMP accumulation is measured in cells pre-treated with NKH477 (an adenylyl cyclase activator) and then exposed to ATI-2341. Receptor internalization is visualized by fluorescence microscopy in cells transiently transfected with CXCR4-eGFP.
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| Animal Protocol |
For ATI-2341 TFA, in BALB/c mice, ATI-2341 is administered intraperitoneally at doses ranging from low to high nmol/kg to assess PMN recruitment into the peritoneum, with peritoneal lavage performed at specific time points for cell counting. For intravenous administration, various doses are injected, and peripheral blood is collected 90 minutes post-injection to measure PMN counts via flow cytometry or complete blood count analysis. Vehicle controls are used for comparison.
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| ADME/Pharmacokinetics |
Detailed PK parameters for ATI-2341 TFA are not fully described in available product documentation. As a pepducin (lipidated peptide), its pharmacokinetic properties differ from small molecules, with potential for rapid distribution. The compound demonstrates in vivo efficacy via both intraperitoneal and intravenous routes, suggesting adequate systemic exposure. More comprehensive PK studies would be needed to determine half-life, clearance, and bioavailability parameters.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for ATI-2341 TFA are not detailed in standard product information. As an allosteric CXCR4 agonist that mobilizes hematopoietic stem cells, potential toxicities may relate to excessive leukocyte mobilization or off-target chemokine receptor activation. Standard laboratory safety precautions should be followed, including proper handling and disposal as per institutional guidelines for peptide-based compounds.
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| References |
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| Additional Infomation |
ATI-2341 TFA is a pepducin (lipidated peptide agonist) targeting CXCR4 with the sequence 1-Oxohexadecyl-MGYQKKLRSMTDKYRL. It has a molecular weight of 2370.84 as the TFA salt and functions as a biased allosteric agonist favoring Galphai activation. This compound represents a novel therapeutic approach for mobilizing hematopoietic stem and progenitor cells prior to autologous bone marrow transplantation. Its discovery was published in PNAS (2010). No clinical approval has been obtained to date.
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| Molecular Formula |
C106H179F3N26O27S2
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| Molecular Weight |
2370.84
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| Related CAS # |
ATI-2341;1337878-62-2
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| Appearance |
White to off-white solid powder
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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 :~50 mg/mL (~21.09 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.05 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 2: ≥ 2.5 mg/mL (1.05 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 | 0.4218 mL | 2.1090 mL | 4.2179 mL | |
| 5 mM | 0.0844 mL | 0.4218 mL | 0.8436 mL | |
| 10 mM | 0.0422 mL | 0.2109 mL | 0.4218 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.
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