| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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Purity: ≥98%
| Targets |
SB-423562 targets the calcium-sensing receptor (CaR), a G protein-coupled receptor that plays a key role in calcium homeostasis. By antagonizing CaR, it mimics the effect of low calcium and stimulates the release of parathyroid hormone (PTH) from the parathyroid gland. This mechanism promotes bone formation.
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| ln Vitro |
In vitro, SB-423562 exhibits strong inhibitory effects on CaR signaling, making it a valuable tool for investigating calcium homeostasis and related metabolic disorders. It potently blocks CaR activation and downstream signaling pathways. The compound's activity is confirmed in cell-based assays measuring CaR-mediated intracellular calcium mobilization or other signaling readouts.
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| ln Vivo |
In vivo, daily oral administration of SB-423557, a related compound, promoted bone formation and improved parameters of bone strength in an ovariectomized rat model of bone loss. In healthy human volunteers, single doses of intravenous SB-423562 elicited transient elevations of endogenous PTH concentrations. Both agents were well tolerated in humans.
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| Enzyme Assay |
The in vitro receptor binding assay for SB-423562 involves competition binding experiments using membranes from cells expressing the calcium-sensing receptor (CaR). Radiolabeled CaR ligands are used to determine the binding affinity of SB-423562. Functional assays measuring CaR-mediated intracellular calcium mobilization or inhibition of PTH release are also performed to confirm antagonist activity.
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| Cell Assay |
In vitro cell-based assays are performed using cell lines that endogenously or heterologously express CaR. Cells are treated with SB-423562 and stimulated with calcium or other CaR agonists. The inhibition of CaR-mediated signaling, such as intracellular calcium mobilization, is measured. IC₅₀ values are determined from dose-response curves.
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| Animal Protocol |
In vivo animal experiments for SB-423562 have been conducted in ovariectomized rat models of bone loss. Animals are administered the compound orally or subcutaneously, and bone mineral density, bone strength parameters, and markers of bone turnover are assessed. PTH levels are measured to confirm target engagement. The compound has also been studied in healthy human volunteers.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SB-423562 have been characterized in preclinical species and humans. It is a short-acting CaR antagonist with rapid clearance. After intravenous administration, it elicits transient PTH release. The compound is well-absorbed and has suitable PK properties for oral administration. Detailed PK parameters include half-life, clearance, and bioavailability.
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| Toxicity/Toxicokinetics |
SB-423562 was well tolerated in humans in early clinical studies. Transient increases in serum calcium, an expected effect of increased PTH concentrations, were observed post-dose at higher doses. No significant safety concerns were reported. Standard toxicology assessments have been conducted to support clinical development.
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| References | |
| Additional Infomation |
SB-423562 represents a novel class of orally administered bone-forming treatments for osteoporosis. It acts as a short-acting CaR antagonist to elicit transient PTH release, mimicking the bone-anabolic effects of intermittent PTH administration. The compound has provided early proof of principle in humans. It has not been approved for clinical use.
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| Exact Mass |
436.236
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|---|---|
| CAS # |
351490-72-7
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| Related CAS # |
351490-72-7 (HCl);351490-27-2;351490-92-1 (sodium);
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| PubChem CID |
68607251
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
33
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| Complexity |
643
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)(CC1CC2=CC=CC=C2C1)NC[C@H](COC3=C(C=CC(=C3)CCC(=O)O)C#N)O
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| InChi Key |
WVXHWCHBKCXTJA-GNAFDRTKSA-N
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| InChi Code |
InChI=1S/C26H32N2O4.ClH/c1-26(2,14-19-11-20-5-3-4-6-21(20)12-19)28-16-23(29)17-32-24-13-18(8-10-25(30)31)7-9-22(24)15-27;/h3-7,9,13,19,23,28-29H,8,10-12,14,16-17H2,1-2H3,(H,30,31);1H/t23-;/m1./s1
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| Chemical Name |
(R)-3-(4-cyano-3-(3-((1-(2,3-dihydro-1H-inden-2-yl)-2-methylpropan-2-yl)amino)-2-hydroxypropoxy)phenyl)propanoic acid hydrochloride
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| Synonyms |
SB-423562 HCl; SB 423562 HCl; SB423562 HCl; NPSP-795; SB-423562; SB-423562-A; SHP-635; SB-423562A; NPSP795; SB423562; SB423562A; SHP635; SB423562A; NPSP 795; SB 423562; SB 423562 A; SHP 635;SB 423562A
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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.) |
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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