| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
SB-756050 selectively targets the TGR5 (GPBAR1) receptor, a bile acid receptor involved in metabolic regulation and energy homeostasis. It acts as a potent agonist with an EC₅₀ of 1.3 μM for the human receptor. It is selective for TGR5 over the farnesoid X receptor (FXR) and a panel of other receptors, channels, and transporters.
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| ln Vitro |
One possible target for the therapy of type 2 diabetes (T2D) is the bile acid receptor TGR5 [1].
In vitro, SB-756050 demonstrates potent agonistic activity at the human TGR5 receptor with an EC₅₀ of 1.3 μM. It activates TGR5-mediated signaling pathways, which are involved in glucose metabolism and insulin secretion. The compound is used in cell-based assays to study TGR5 activation and its downstream effects. |
| ln Vivo |
The drug SB756050 was well-tolerated; when combined with sitagliptin, it did not significantly alter exposure and showed nonlinear pharmacokinetics, with less than dose-proportional increases in plasma exposure above 100 mg. Between and between dose groups, SB756050's pharmacodynamic effects were remarkably inconsistent, with the two lowest doses causing an increase in glucose and the two highest doses causing no decrease in glucose. SB 756050 Despite having a distinct intestinal hormone plasma profile, sitagliptin's effects on glucose are similar to those of sitagliptin alone [1].
In vivo, SB-756050 (10-100 mg/kg) decreases fasting glucose levels and increases glucose disposal rate and insulin secretion in diabetic Goto Kakizaki rats. In patients with type 2 diabetes, it demonstrated highly variable pharmacodynamic effects, with increases in glucose seen at lower doses and no reduction at higher doses. It was well-tolerated in clinical studies. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for SB-756050 typically involves radioligand binding or functional assays using membranes from cells expressing the human TGR5 receptor. Competition binding experiments are performed with a labeled TGR5 ligand to determine the affinity and potency of SB-756050. Functional assays measure TGR5-mediated cAMP accumulation or β-arrestin recruitment.
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| Cell Assay |
In vitro cell-based assays are conducted using cell lines engineered to express human TGR5. Cells are treated with SB-756050 at various concentrations, and TGR5 activation is measured via downstream signaling readouts such as cAMP production or changes in gene expression. EC₅₀ values are calculated from dose-response curves. Cytotoxicity and cell viability are also assessed.
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| Animal Protocol |
In vivo animal experiments for SB-756050 have been performed in diabetic Goto Kakizaki rats. Animals are administered the compound orally or via other routes, and blood glucose levels, insulin secretion, and glucose disposal rate are measured. Pharmacodynamic effects are assessed over time. The compound has also been studied in clinical trials involving patients with type 2 diabetes.
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| ADME/Pharmacokinetics |
In clinical pharmacokinetic studies, SB-756050 is readily absorbed and exhibits nonlinear pharmacokinetics with a less than dose-proportional increase in plasma exposure above 100 mg. It shows no significant changes in exposure when co-administered with sitagliptin. The compound is well-tolerated with a favorable safety profile in patients.
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| Toxicity/Toxicokinetics |
In clinical studies, SB-756050 was well-tolerated with no significant safety concerns reported. Standard toxicology assessments have been conducted to support clinical development. The compound demonstrated acceptable safety margins in preclinical species. It is intended for research use only and has been evaluated in phase 1 clinical trials.
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| References | |
| Additional Infomation |
SB-756050 is a selective TGR5 agonist that has been investigated for the treatment of type 2 diabetes. It was evaluated in a phase 1 clinical trial in patients with T2D to assess safety, pharmacokinetics, and pharmacodynamic effects. Despite being well-tolerated, it demonstrated highly variable glucose effects and did not show consistent glucose-lowering efficacy. It is not approved for clinical use.
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| Molecular Formula |
C21H28N2O8S2
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|---|---|
| Molecular Weight |
500.58562374115
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| Exact Mass |
500.128
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| Elemental Analysis |
C, 50.39; H, 5.64; N, 5.60; O, 25.57; S, 12.81
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| CAS # |
447410-57-3
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| PubChem CID |
1520267
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
653.1±65.0 °C at 760 mmHg
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| Flash Point |
348.8±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
758
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(N1CCN(S(=O)(C2=CC=C(OC)C(OC)=C2)=O)CCC1)(C3=CC=C(OC)C(OC)=C3)=O
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| InChi Key |
GJUFPAZNBPFNRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H28N2O8S2/c1-28-18-8-6-16(14-20(18)30-3)32(24,25)22-10-5-11-23(13-12-22)33(26,27)17-7-9-19(29-2)21(15-17)31-4/h6-9,14-15H,5,10-13H2,1-4H3
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| Chemical Name |
1,4-bis((3,4-dimethoxyphenyl)sulfonyl)-1,4-diazepane
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| Synonyms |
SB-756050; SB 756050; SB756050
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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) |
DMSO : ≥ 150 mg/mL (~299.65 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 | 1.9976 mL | 9.9882 mL | 19.9764 mL | |
| 5 mM | 0.3995 mL | 1.9976 mL | 3.9953 mL | |
| 10 mM | 0.1998 mL | 0.9988 mL | 1.9976 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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