| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
AT-1015 HCl primarily targets the 5-HT2A serotonin receptor, a subtype of the 5-HT2 receptor family which belongs to the G protein-coupled receptor superfamily. It acts as a potent antagonist at this receptor with a pKi of 7.94. By blocking 5-HT2A receptors on vascular smooth muscle and platelets, the compound inhibits serotonin-mediated vasoconstriction and platelet aggregation. This receptor is involved in various physiological processes including vascular tone regulation and thrombus formation.
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| ln Vitro |
In vitro, AT-1015 selectively inhibits 5-HT2A receptor-mediated platelet aggregation. Its activity in this assay is approximately equivalent to that of ketanserin (a 5-HT2A/2C receptor antagonist) and is reported to be 100 times more potent than sarpogrelate (another 5-HT2A receptor antagonist). The compound effectively blocks 5-HT2A receptor-mediated vasoconstriction in various in vitro preparations. These in vitro findings demonstrate its high potency and selectivity for the 5-HT2A receptor subtype over other related receptors.
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| ln Vivo |
In vivo, AT-1015 has demonstrated efficacy in several animal models. It prolongs clotting time in a rat model of thrombus formation. Additionally, the compound ameliorates laurate-induced peripheral vascular lesions in rodents. These effects are consistent with its mechanism of blocking 5-HT2A receptors, thereby preventing serotonin-induced vasoconstriction and platelet aggregation. The compound has also been evaluated in a randomized trial for the treatment of intermittent claudication, although this study did not demonstrate significant efficacy in patients.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for AT-1015 typically involves radioligand binding displacement studies using membrane preparations from cells expressing the human 5-HT2A receptor. The compound's affinity (pKi) is determined by measuring its ability to displace a specific radiolabeled ligand from the receptor. These cell-free assays allow for the direct assessment of receptor binding affinity without the confounding factors of cellular metabolism or signaling pathways, providing a clear measure of the compound's intrinsic affinity for the 5-HT2A receptor.
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| Cell Assay |
In vitro cellular assays for AT-1015 typically utilize platelet-rich plasma or washed platelet preparations to assess its functional antagonism. Platelet aggregation is induced by serotonin (5-HT) in the presence of other agonists such as collagen, ADP, epinephrine, or thrombin, which potentiate the 5-HT response. The compound's ability to selectively inhibit 5-HT2A receptor-mediated aggregation is then measured. These assays quantify the inhibitory effect of AT-1015 on platelet function, demonstrating its functional antagonism at the 5-HT2A receptor in a relevant cell type.
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| Animal Protocol |
In vivo animal studies for AT-1015 have been conducted in rat models. One key model involves the laurate-induced peripheral vascular lesion model, where the compound's ability to ameliorate vascular damage is assessed. Another model is the rat arterial thrombosis model, used to evaluate its antithrombotic activity and effects on bleeding time. In these studies, AT-1015 is typically administered via various routes, and endpoints such as thrombus formation, vascular lesion severity, and clotting parameters are measured to evaluate its in vivo efficacy.
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| ADME/Pharmacokinetics |
AT-1015 HCl is a long-acting 5-HT2A receptor antagonist. Its pharmacokinetic properties are characterized by its ability to maintain receptor blockade over an extended period, which is a key feature distinguishing it from other antagonists in its class. The compound's formulation as a hydrochloride salt enhances its aqueous solubility for administration. However, detailed pharmacokinetic parameters such as half-life, volume of distribution, and bioavailability are not extensively detailed in the available literature. Its long-acting nature suggests favorable metabolic stability and/or sustained receptor binding.
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| Toxicity/Toxicokinetics |
Specific toxicity data for AT-1015 HCl are not extensively detailed in the available literature. However, as a 5-HT2A receptor antagonist, its safety profile is likely related to its pharmacological activity. In clinical studies for intermittent claudication, the compound was evaluated for safety, although the specific adverse event profile is not detailed in the search results. Preclinical toxicology studies would typically be conducted to assess the compound's safety margin, but these specific data are not provided. As a research compound, its toxicity profile would be evaluated in standard in vitro and in vivo models.
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| References |
: Komiyama T, Kihara H, Hirose K, Yoshimoto R, Shigematsu H. AT-1015, a novel serotonin2A receptor antagonist, improves resaturation of exercised ischemic muscle in hypercholesterolemic rabbits. J Vasc Surg. 2004 Mar;39(3):661-7.
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| Additional Infomation |
AT-1015 is an organic molecular entity.
AT-1015 HCl is a research compound that has been investigated for therapeutic applications. It was evaluated in a randomized trial for the treatment of intermittent claudication, a condition characterized by muscle pain due to inadequate blood flow, where serotonin was hypothesized to contribute to symptoms via microvascular vasoconstrictor and thrombotic effects. However, this clinical study did not demonstrate efficacy. The compound remains a valuable tool for studying 5-HT2A receptor function and the role of serotonin in vascular and platelet biology. It is not approved for clinical use and is intended for research purposes only. |
| Molecular Formula |
C29H34CLN3O2
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|---|---|
| Molecular Weight |
492.052166461945
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| Exact Mass |
491.233
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| CAS # |
190508-50-0
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| PubChem CID |
9805663
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
35
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| Complexity |
744
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.O=C(C1CCN(C=O)CC1)NCCN1CC/C(=C2/C3C=CC=CC=3C=CC3=CC=CC=C/23)/CC1
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| InChi Key |
YZHGXYNLMHGNJZ-UHFFFAOYSA-N
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| InChi Code |
1S/C29H33N3O2.ClH/c33-21-32-18-13-25(14-19-32)29(34)30-15-20-31-16-11-24(12-17-31)28-26-7-3-1-5-22(26)9-10-23-6-2-4-8-27(23)28/h1-10,21,25H,11-20H2,(H,30,34)1H
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| Chemical Name |
4-Piperidinecarboxamide,
N-(2-(4-(5H-dibenzo(a,d)cyclohepten-5-ylidene)-1-piperidinyl)ethyl)-1-formyl-,
hydrochloride (1
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| Synonyms |
AT1015 AT 1015 HCl, AT-1015 hydrochloride anhydrous
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0323 mL | 10.1616 mL | 20.3231 mL | |
| 5 mM | 0.4065 mL | 2.0323 mL | 4.0646 mL | |
| 10 mM | 0.2032 mL | 1.0162 mL | 2.0323 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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