| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vivo |
In rats, BAY 73-1449 (0.1–1 mg/kg; iv) significantly lowers splenic shunt channel outflow but not mesenteric inflow [1]. On the degree of portosystemic shunting in rats, BAY 73-1449 (1–5 mg/kg, subcutaneous injection, once daily, for 7 days) shows no effect [1]. Rats' portal pressure is unaffected by BAY 73-1449 (1 mg/kg, subcutaneous injection once daily for 7 days) [1].
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats (250-350 g) with portal vein ligation [1]
Doses: 0.1, 1 mg/kg Route of Administration: Single intravenous (iv) (iv)injection Experimental Results: Dramatically diminished shunt blood flow without affecting mesenteric blood flow. For acute studies, male Wistar rats (250-350 g) underwent portal vein ligation surgery under ether anesthesia. Seven days post-ligation, animals were re-anesthetized with ether, the jugular vein and carotid artery were cannulated, and anaesthesia was maintained with intravenous pentobarbitone. The abdomen was re-opened, and a shunt vessel (running from spleen to renal vein) was carefully placed on a plastic vessel holder attached to a laser Doppler flow probe to measure blood flow. Mesenteric arterial blood flow was also recorded in some experiments. Following a 15-minute stabilization period, BAY 73-1449 (0.1-1 mg/kg) or an equivalent volume of saline (1 ml/kg) was infused intravenously over 1 minute and washed in with saline. Blood pressure and flow were measured 2 minutes after injection. Responses were expressed as percentage changes in vascular conductance (flow signal change divided by mean arterial pressure change) [1]. For chronic studies, animals were treated subcutaneously with BAY 73-1449 (1 or 5 mg/kg) or an equivalent volume of saline once daily for 7 days, beginning just before portal vein ligation. Seven days after surgery, the degree of porto-systemic shunting was assessed using the radioactive microsphere technique. Animals were re-anesthetized with ether, the abdomen was re-opened, and approximately 100,000 ⁵⁷Co radioactive microspheres (15 μm diameter) suspended in 10% dextran were injected directly into the spleen. After 2 minutes, the animal was killed, and the lungs, liver, spleen, and kidneys were removed for radioactivity counting. The percentage shunting was calculated as: (lung cpm × 100) / (lung cpm + liver cpm) [1]. For portal pressure measurement, seven days after portal vein ligation, animals were re-anesthetized with ether, the abdomen was opened, and a 21-gauge needle attached to a blood pressure transducer was introduced into the portal vein. The stable pressure reading was taken as portal pressure [1]. |
| References |
| Molecular Formula |
C26H23N3O3
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|---|---|
| Molecular Weight |
425.47912
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| Exact Mass |
425.173
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| CAS # |
693790-96-4
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| PubChem CID |
9910289
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| Appearance |
White to off-white solid powder
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| LogP |
5.2
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
32
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| Complexity |
555
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(COC2C=CC(C3N=CN=C(NC(C(O)=O)CC4C=CC=CC=4)C=3)=CC=2)C=CC=CC=1
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| InChi Key |
RRYFPNITZGCUPZ-XMMPIXPASA-N
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| InChi Code |
InChI=1S/C26H23N3O3/c30-26(31)24(15-19-7-3-1-4-8-19)29-25-16-23(27-18-28-25)21-11-13-22(14-12-21)32-17-20-9-5-2-6-10-20/h1-14,16,18,24H,15,17H2,(H,30,31)(H,27,28,29)/t24-/m1/s1
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| Chemical Name |
(2R)-3-phenyl-2-[[6-(4-phenylmethoxyphenyl)pyrimidin-4-yl]amino]propanoic acid
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| Synonyms |
BAY-73-1449 BAY 73-1449 BAY73-1449
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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 : ~250 mg/mL (~587.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.89 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.89 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 20.8 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 | 2.3503 mL | 11.7514 mL | 23.5029 mL | |
| 5 mM | 0.4701 mL | 2.3503 mL | 4.7006 mL | |
| 10 mM | 0.2350 mL | 1.1751 mL | 2.3503 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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