| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
GPRC5A[1]
GPRC5A (G protein-coupled receptor class C group 5 member A). 7-Fluorotryptamine hydrochloride is a potent synthetic agonist of GPRC5A. It induces GPRC5A-mediated β-arrestin recruitment with an EC50 of 7.2 μM. By activating this receptor, the compound can be used to study its role in various signaling pathways, particularly those related to immunity and cancer. |
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| ln Vitro |
7-Fluorotryptamine (100 μM) hydrochloride causes GPRC5A to recruit β-arrestin in the PRESTO-Tango assay [1]. Treatment of WT and GPRC5A-KO cells with 50 μM, 8-hour hydrochloride of 7-fluorotryptamine hydrochloride can downregulate TNFα-induced genes (e.g., IL41A, CXCL10, CSF2) [1]. HTLA and HT-29 cells do not exhibit any toxicity when exposed to 7-fluorotryptamine hydrochloride (0-100 μM, 16 h) [1].
7-Fluorotryptamine hydrochloride is a potent agonist of GPRC5A, with an EC50 of 7.2 μM for inducing GPRC5A-mediated β-arrestin recruitment. At a concentration of 100 μM, it causes GPRC5A to recruit β-arrestin in the PRESTO-Tango assay. Its activity is specific to GPRC5A, as other fluoro-substituted tryptamines do not show this activity. |
| ln Vivo |
In vivo, 7-Fluorotryptamine hydrochloride would be used to study the physiological and pathophysiological roles of GPRC5A. As a selective agonist, it could be administered to animal models to investigate the effects of GPRC5A activation on various processes, such as immune responses or cancer progression. Its in vivo effects would be determined by assessing changes in relevant biomarkers and disease phenotypes.
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| Enzyme Assay |
In vitro studies for GPRC5A agonists like 7-Fluorotryptamine hydrochloride typically involve receptor binding and functional assays. Radioligand binding assays can be used to measure the compound's affinity for GPRC5A. Functional assays, such as the PRESTO-Tango assay or β-arrestin recruitment assays, are used to confirm its agonistic activity and determine its potency (EC50).
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| Cell Assay |
Cellular assays are used to characterize the activity of 7-Fluorotryptamine hydrochloride. Cells expressing GPRC5A are treated with the compound, and the recruitment of β-arrestin is measured as a readout of receptor activation. This is typically done using a cell-based assay system like PRESTO-Tango, where receptor activation leads to a measurable signal, allowing for the determination of the compound's EC50 of 7.2 μM.
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| Animal Protocol |
In vivo studies with 7-Fluorotryptamine hydrochloride would be performed in animal models to explore GPRC5A function. Depending on the research focus, the compound could be administered to study its effects on immune cell function, tumor growth, or other GPRC5A-mediated processes. The compound's ability to activate GPRC5A in vivo would be confirmed by measuring downstream signaling or physiological responses.
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| ADME/Pharmacokinetics |
7-Fluorotryptamine hydrochloride is a small molecule (molecular weight: 214.65) that is soluble in DMSO. Its pharmacokinetic properties, such as oral bioavailability and brain penetration, would be key factors for its utility in in vivo studies. As a tryptamine derivative, it may have properties that allow it to cross the blood-brain barrier, which could be relevant for studying GPRC5A in the central nervous system.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for 7-Fluorotryptamine hydrochloride. As a research compound, its safety profile would need to be established through standard toxicological studies. Given its mechanism of action as a GPRC5A agonist, potential toxicities would be related to the biological functions of this receptor, which are still being elucidated.
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| References | |
| Additional Infomation |
7-Fluorotryptamine hydrochloride (CAS#: 159730-09-3) is a potent synthetic agonist of GPRC5A. It induces GPRC5A-mediated β-arrestin recruitment with an EC50 of 7.2 μM. It is a valuable research tool for studying GPRC5A signaling in immune and cancer pathways. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C10H12CLFN2
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|---|---|
| Molecular Weight |
214.67
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| Exact Mass |
214.067
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| CAS # |
159730-09-3
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| PubChem CID |
53487481
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| Appearance |
White to off-white solid powder
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| LogP |
3.31
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
14
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| Complexity |
174
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C(=C1)F)NC=C2CCN.Cl
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| InChi Key |
JWAZOMQARDNFMN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H11FN2.ClH/c11-9-3-1-2-8-7(4-5-12)6-13-10(8)9;/h1-3,6,13H,4-5,12H2;1H
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| Chemical Name |
2-(7-fluoro-1H-indol-3-yl)ethanamine;hydrochloride
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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: 125 mg/mL (582.29 mM)
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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 | 4.6583 mL | 23.2916 mL | 46.5831 mL | |
| 5 mM | 0.9317 mL | 4.6583 mL | 9.3166 mL | |
| 10 mM | 0.4658 mL | 2.3292 mL | 4.6583 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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