| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Retinoid X Receptor (RXR) pan-agonist [2]
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|---|---|
| ln Vitro |
It was discovered that SR11237 was unsuccessful at the retinoic acid receptor but could successfully transactivate the chloramphenicol acetyltransferase reporter gene through RXR using a nuclear receptor co-transfection experiment in COS-1 cells [1].
Culturing newborn mouse tibiae with SR 11237 at a concentration of 5 μM for 4 days resulted in a significant decrease in longitudinal bone growth compared to treatment with 1 μM SR 11237 [2] |
| ln Vivo |
On postpartum days 5 to 15, SR11237 (BMS-649) (25 mg/kg; i.p.; daily) induces irregular ossification and premature growth plate closure [2].
Daily intraperitoneal injection of SR 11237 (25 mg/kg) from postnatal day 5 to 15 in rats resulted in a 30% reduction in body weight in both male and female pups at P16 compared to DMSO-injected controls [2] The same treatment regimen significantly shortened the length of femur, tibia, and radius bones in female rats, and shortened all four measured long bones (humerus, tibia, femur, and radius) in male rats at P16 [2] MicroCT analysis revealed that SR 11237-treated male rats had thinner, osteopenic-looking fore- and hindlimbs, dysmorphic/undercalcified metacarpals and metatarsals, and disrupted secondary ossification centers compared to controls [2] Histological analysis (Safranin O/Fast Green staining) of long bones from SR 11237-treated rats showed severely disturbed growth plate organization, premature closure of the growth plate, and apparent fusion of the primary and secondary ossification centers [2] Immunohistochemistry on tibial sections from SR 11237-treated rats showed reduced numbers of PCNA-positive (proliferating) and P57-positive (pre-hypertrophic) chondrocytes, disorganized SOX9-positive cell distribution surrounding calcified tissue, intense TRAP staining throughout the central epiphysis indicating increased osteoclast activity, and increased TUNEL staining at the osteo-chondral junction [2] |
| Animal Protocol |
Animal/Disease Models: SD (SD (Sprague-Dawley)) rat [2]
Doses: 25 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day on postpartum days 5 to 15 Experimental Results: Caused ossification and bone morphology disorders in rats, including premature growth plate closure and infiltration of ossified tissue through the central epiphysis. Sprague-Dawley rat pups were randomly divided into two groups. One group received daily intraperitoneal injections of SR 11237 at a dose of 25 mg per kg body weight, dissolved in DMSO. The control group received an equal volume of DMSO vehicle. Injections were administered once daily from postnatal day 5 to postnatal day 15. All animals were harvested on postnatal day 16 for analysis [2] For the ex vivo organ culture model, tibiae were harvested from newborn CD1 mice and cultured in serum-free α-MEM medium supplemented with bovine serum albumin, L-glutamine, β-glycerophosphate, ascorbic acid, and penicillin-streptomycin. On culture days 1 and 3, the medium was replaced, and bones were treated with DMSO (control) or SR 11237 at concentrations of 0.1, 1, or 5 μM. Bones were cultured for a total of 4 days [2] |
| References |
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| Additional Infomation |
SR 11237 is described as a selective RXR (retinol X receptor) pan-agonist [2]. Studies have shown that SR 11237 activation of the RXR during early postnatal development leads to abnormal ossification, premature closure of the growth plate, and reduced longitudinal bone growth in rodents. These observed effects may involve chondrocyte exit from the cell cycle and increased osteoclast activity and bone formation, ultimately leading to fusion of ossification centers [2]. The 25 mg/kg dose used in rat studies is reportedly similar to previous in vivo doses of this compound [2].
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| Molecular Formula |
C24H28O4
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|---|---|
| Molecular Weight |
380.476727485657
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| Exact Mass |
380.199
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| Elemental Analysis |
C, 75.76; H, 7.42; O, 16.82
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| CAS # |
146670-40-8
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| Related CAS # |
146670-40-8 (SR 11237); 121346-32-5 (SR-33805)
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| PubChem CID |
127019
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| Appearance |
White to off-white solid powder
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| Density |
1.139g/cm3
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| Boiling Point |
499.9ºC at 760 mmHg
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| Flash Point |
167.1ºC
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| Vapour Pressure |
8.16E-11mmHg at 25°C
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| Index of Refraction |
1.561
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| LogP |
4.981
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
581
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1CCOC1(C1C=CC(C(=O)O)=CC=1)C1C=CC2=C(C=1)C(C)(C)CCC2(C)C
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| InChi Key |
ZZUKALQMHNSWTK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H28O4/c1-22(2)11-12-23(3,4)20-15-18(9-10-19(20)22)24(27-13-14-28-24)17-7-5-16(6-8-17)21(25)26/h5-10,15H,11-14H2,1-4H3,(H,25,26)
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| Chemical Name |
4-(2-(5,6,7,8-Tetrahydro-5,5,8,8,-tetramethyl-2-naphthalenyl)-1,3-dioxolan-2-yl)benzoic acid
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| Synonyms |
SR 11237; SR11237; SR-11237; BMS 649; BMS-649.
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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 : ~5 mg/mL (~13.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL | |
| 5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL | |
| 10 mM | 0.2628 mL | 1.3141 mL | 2.6283 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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