| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
BA 1 TFA targets the bombesin (BB) receptor family, specifically binding with high affinity to three subtypes: bombesin receptor subtype 3 (BRS3/BB3), gastrin-releasing peptide receptor (GRPR/BB1), and neuregulin B receptor (NMBR/BB2). These receptors are G protein-coupled receptors (GPCRs) that mediate diverse biological processes including gastrointestinal hormone release, satiety, circadian rhythm control, and thermoregulation, and they are often overexpressed in various tumors.
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|---|---|
| ln Vitro |
BA1 (0.1 μM) dramatically raises the tyrosine phosphorylation of FAK in NCI-H1299 cells transfected with BRS-3[1]
In vitro, BA 1 TFA binds to BRS3, GRPR, and NMBR with high affinity, with IC50 values of 6 nM (BRS3), 0.4 nM (GRPR), and 2.5 nM (NMBR). It enhances glucose transport in primary myocytes derived from obese and diabetic animal models. Additionally, BA 1 (0.1 microM) significantly increases the tyrosine phosphorylation of FAK in BRS-3-transfected NCI-H1299 lung cancer cells and stimulates the proliferation of these cells in vitro. |
| ln Vivo |
In vivo, BA 1 TFA has been shown to enhance glucose transport in primary myocytes from obese and diabetic animal models, indicating its potential role in metabolic regulation. However, detailed in vivo pharmacokinetic and efficacy studies for this compound are limited in the available literature, with most data derived from in vitro cell-based assays and binding studies.
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| Enzyme Assay |
For BA 1 TFA, enzyme/receptor binding is typically assessed using radioligand binding assays on membrane preparations from cells expressing recombinant bombesin receptors (BRS3, GRPR, NMBR). Various concentrations of BA 1 TFA are incubated with receptor membranes and a labeled tracer (e.g., [125I]-Tyr4-bombesin). Specific binding is measured after filtration or centrifugation, and IC50 values are calculated from competition curves. For BRS3, the reported IC50 is 6 nM.
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| Cell Assay |
For BA 1 TFA, NCI-H1299 lung cancer cells (transfected with BRS-3 receptor or wild-type) are cultured in appropriate medium. Cells are treated with BA 1 (0.1 microM) and incubated. Cell lysates are collected, and FAK tyrosine phosphorylation is analyzed by immunoblotting with anti-phospho-FAK antibodies. Alternatively, cell proliferation is assessed using standard viability assays. Vehicle controls and appropriate positive controls are included in all experiments.
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| Animal Protocol |
For BA 1 TFA, detailed animal model protocols are not fully described in available literature. However, based on related bombesin receptor agonists, in vivo studies may involve administration to rodent models (mice or rats) to assess metabolic effects such as glucose transport enhancement. Dosages and administration routes are typically determined based on pilot studies, with endpoints including blood glucose measurement and tissue analysis of receptor-mediated signaling pathways.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for BA 1 TFA are not extensively detailed in standard product literature. As a bombesin receptor agonist peptide, it is likely to have limited oral bioavailability and may require parenteral administration for in vivo studies. Preclinical PK parameters such as half-life, clearance, volume of distribution, and bioavailability would need to be determined experimentally for specific animal models.
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| Toxicity/Toxicokinetics |
Available literature does not provide extensive toxicological data for BA 1 TFA. As a research-use peptide agonist, standard handling precautions should be observed. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and safety pharmacology would be required for therapeutic development. For laboratory research, standard biosafety practices for peptide handling should be followed.
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| References | |
| Additional Infomation |
BA 1 TFA is a peptide agonist with the sequence YQWAV(Bal)HF(Nle)-NH2 (with modifications including D-Tyr, beta-Ala, and Nle) and a molecular weight of 1247.32 as the TFA salt. The free base (BA 1, CAS 183241-31-8) has a molecular weight of 1133.32. It is provided as a TFA salt for improved solubility and stability. This compound is a potent bombesin receptor family agonist with high affinity for all three bombesin receptor subtypes. It is used exclusively for research purposes and not for human therapy.
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| Molecular Formula |
C59H77F3N14O13
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|---|---|
| Molecular Weight |
1247.32
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| Exact Mass |
1132.582
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| Related CAS # |
BA 1;183241-31-8
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| PubChem CID |
91826107
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
14
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| Rotatable Bond Count |
32
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| Heavy Atom Count |
82
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| Complexity |
2160
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CCCC[C@@H](C(=O)N)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC2=CN=CN2)NC(=O)[C@H](C)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@@H](CC5=CC=C(C=C5)O)N
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| InChi Key |
BXSSCSKCOFKPOK-ZWAOGYCRSA-N
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| InChi Code |
InChI=1S/C57H76N14O11/c1-6-7-16-42(49(60)74)66-55(80)44(25-34-13-9-8-10-14-34)69-56(81)46(27-37-29-61-30-63-37)68-50(75)32(4)65-57(82)48(31(2)3)71-51(76)33(5)64-54(79)45(26-36-28-62-41-17-12-11-15-39(36)41)70-53(78)43(22-23-47(59)73)67-52(77)40(58)24-35-18-20-38(72)21-19-35/h8-15,17-21,28-33,40,42-46,48,62,72H,6-7,16,22-27,58H2,1-5H3,(H2,59,73)(H2,60,74)(H,61,63)(H,64,79)(H,65,82)(H,66,80)(H,67,77)(H,68,75)(H,69,81)(H,70,78)(H,71,76)/t32-,33-,40+,42-,43-,44-,45-,46-,48-/m0/s1
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| Chemical Name |
(2S)-2-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxohexan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]pentanediamide
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 | 0.8017 mL | 4.0086 mL | 8.0172 mL | |
| 5 mM | 0.1603 mL | 0.8017 mL | 1.6034 mL | |
| 10 mM | 0.0802 mL | 0.4009 mL | 0.8017 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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