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CAS NO.145040-37-5
98%(500-1000)Kilogram98%(100-500)Metric Ton
| Molecular Formula | C33H34N6O6 |
| Molar Mass | 610.66 |
| Density | 1.37±0.1 g/cm3(Predicted) |
| Melting Point | 168-170 C |
| Boling Point | 843.3±75.0 °C(Predicted) |
| Solubility | Soluble in water (<1 mg/ml at 25 °C), DMSO (122 mg/ml at 25 °C), methanol, DMF (~30 |
| Appearance | powder |
| Color | white to beige |
| Maximum wavelength(λmax) | ['304nm(EtOH)(lit.)'] |
| Merck | 14,1739 |
| pKa | pKa 3.55 (H2O t=25.0 I=0.025) (Uncertain);5.91(H2O t=25.0 I=0.025) (Uncertain) |
| Storage Condition | 2-8°C |
| Sensitive | Sensitive to heat |
| Refractive Index | 1.665 |
| MDL | MFCD00871371 |
| Use | Uses: pesticides and pharmaceutical intermediates |
chloride
take 0.40g of this product, add 0801 of water, strongly shake for 10 minutes, filter, take 25ml of filtrate, check according to law (general rule), and standard sodium chloride solution 5.0ml of the control solution should not be deeper (0.05%).
Related substances
take about 20mg of this product, put it in a 50ml measuring flask, add acetonitrile-water (3:2) to dissolve and dilute to the scale, shake well, as a test solution; 1 ml was accurately measured, placed in a 100ml measuring flask, diluted to the scale with acetonitrile-water (3:2), and shaken to serve as a control solution. Using octadecyl cinnamate-bonded cinnamate as filler (Ecosd C18 column or Kromasil100-5 C18 column, 0512 × 4.6) as determined by HPLC (general), 5pm or performance equivalent column); Acetonitrile-glacial acetic acid-water (57:1:43) as mobile phase A, acetonitrile-glacial acetic acid-water (90:1:10) mobile Phase B, the detection wavelength was 254nm. Gradient elution was performed as follows. Take 20ml of test solution and add 0.lmol/L hydrochloric acid solution l. 0ML, 90°C water bath heating for 10 minutes, add 0.1.0mL of 1 mol/L sodium hydroxide solution was neutralized and used as the system applicable solution, 10u1 was injected into the liquid chromatograph, and the chromatogram was recorded. The peak retention time of Candesartan Cilexetil was about 20 minutes, (±)-1 -[(cyclohexyloxy) carbonyloxy] ethyl 2-oxotetrazol-5-yl) biphenyl-4-yl] methyl]-2, the relative retention time of 3-dihydro-1h-benzimidazole-4-carboxylate (impurity I) is about 0.6; The number of theoretical plates is not less than 12 000 in terms of Candesartan Cilexetil peak, and the tailing factor should not exceed 1.5. Accurately take 10ul of each sample solution and control solution into the liquid chromatograph, record the chromatogram, if there are impurity peaks in the chromatogram of the sample solution, the Peak area of impurity I shall not be greater than 0.3 times (0.3%) of the main peak area of the control solution, and the peak area of other individual impurities shall not be greater than 0.2 times (0.2%) of the main peak area of the control solution, the sum of each impurity peak area shall not be greater than 0.6 times (0.6%) of the main peak area of the control solution. The peaks in the chromatogram of the test solution which were 0.05 times smaller than the main peak area of the control solution were ignored.
| The prodrug of the antihypertensive drug candesartan-candesartan cilexetil | Hypertension due to its high incidence, high disability rate, High mortality, and the resulting medical, social, family, economic and other burdens, make hypertension from a simple personal illness to a serious social problem. The research and development of first-line drugs for the treatment of hypertension has increasingly become the focus of competition among major manufacturers in the world. The main purpose of treating hypertension is to minimize the total risk of cardiovascular death and disability. The goal of antihypertensive treatment is to restore blood pressure to below 140/90mmHg. At present, there are many clinical antihypertensive drugs, mainly five types, namely diuretics, β-blockers, angiotensin converting enzyme inhibitors (ACE-I), calcium antagonists, and α-blockers. They have certain limitations and side effects in use. Since the 1980s, ACE-I has been widely used in the treatment of various cardiovascular diseases, and has been proved to have a good antihypertensive effect on hypertension. However, because ACE-I also inhibits the degradation of bradykinin, patients often suffer from dry cough during treatment. At present, a new type of antihypertensive drug-angiotensin II receptor antagonism has been on the market one after another. The typical representatives of this type of drug are the losatran of Merck, the valsartan of Novartis, and the eprosartan of SmithKline. Because the effect of this type of drug is more specific than ACE-I, it increases its antihypertensive effect and reduces side effects and does not cause cough, as well as vascular, kidney and cardioprotective effects. This type of drug has become the market for hypertension drugs. Competitive protagonist. Candesartan cilexetil is a prodrug of candesartan, the intensity of action is 10 times that of losartan, the selectivity of action is good (the affinity for AT1 receptor is more than 10000 times higher than AT2), and the action time is long (Take the medicine once a day). Because it is a prodrug that releases activity in the body after oral administration, it is relatively gentle, so it is an ideal hypertension treatment drug. Foreign countries predict that the annual sales volume of this product can reach 2 billion US dollars, so the development of this product will surely achieve good economic and social benefits. |
| candesartan ester tablets | [properties] this product is white or white-like tablets. [Pharmacology and Toxicology] Candesartan cilexetil is rapidly hydrolyzed into the active metabolite candesartan in the body. Candesartan is a selective angiotensin II receptor (AT1) antagonist, which is linked to vascular smooth muscle AT1 receptor Binding to antagonize the vasoconstriction of angiotensin II, thereby reducing peripheral vascular resistance. It is also believed that candesartan can exert a certain antihypertensive effect by inhibiting the secretion of aldosterone by the adrenal glands. Candesartan does not inhibit kininase II and does not affect bradykinin degradation. Experiments conducted in patients with hypertension show that patients taking this product many times can increase plasma renin activity, angiotensin 1 concentration and angiotensin II concentration; taking this product 2-8mg once a day continuously can make Systolic pressure and diastolic pressure decrease, left ventricular myocardial weight and peripheral vascular resistance are reduced, but there is no significant effect on cardiac output, ejection fraction, renal vascular resistance, renal blood flow, and glomerular filtration rate; it has no effect on cerebral blood flow in patients with primary hypertension with cerebrovascular disorders. Toxicological study: Mice, rats and dogs received a single oral dose of candesartan cilexetil 2000mg/kg without death. The maximum tolerance of NIH mice is as high as 6750mg/kg, and the non-toxic dose of this product is 10mg/kg for rats for long-term (26 weeks) oral administration. D, the non-toxic dose of this product for long-term oral administration of Bigger dogs is 20mg/kg. d. Mutagenic, carcinogenic, and reproductive damage tests prove that candesartan cilexetil has been mutagenic by microorganisms, chromosome aberrations, and mammalian DNA gene mutation tests to prove that this product has no mutagenic effect. Rats and mice were given 300 and 1000 mg/kg respectively. D No carcinogenic effect was found for 2 consecutive years (104 weeks) (this dose is 7 times and 70 times of the maximum daily recommended dose of 32mg/d). Female and male rats take this product orally at 300mg/kg. d (83 times the maximum daily recommended dose) has no effect on fertility and fecundity. Reproductive and embryonic toxicity tests showed that 10mg/kg was orally administered to late pregnancy and lactating rats. D this product reduces the survival number of offspring and increases the incidence of hydronephrosis (for the recommended maximum dose of 2. 8 times). Pregnant rabbits take this product orally at 3 mg/kg. D (about 1 of the maximum dose for human use. 7 times), produce maternal toxicity (weight loss or death), but it has no adverse effect on the survival rate, weight, shape, internal organs and bone development of the surviving mother and fetus. Give this product orally to pregnant mice until 1000mg/kg. D (about 138 times the recommended maximum dose for human use) did not see maternal toxicity and fetal dysplasia. |
CAS:
145040-37-5
MF:
C33H34N6O6
MW:
610.66
EINECS:
627-030-2
MDL No.:
MFCD00871371
Melting point:
168-170 C
Boiling point:
843.3±75.0 °C(Predicted)
Density
1.37±0.1 g/cm3(Predicted)
storage temp.
2-8°C
solubility
DMSO: ≥15mg/mL
form
powder
pka
pKa 3.55 (H2O t=25.0 I=0.025) (Uncertain);5.91(H2O t=25.0 I=0.025) (Uncertain)
color
white to beige
λmax
304nm(EtOH)(lit.)
Merck
14,1739
BCS Class
2
InChIKey
GHOSNRCGJFBJIB-UHFFFAOYSA-N
SMILES
C1(OCC)N(CC2=CC=C(C3=CC=CC=C3C3=NNN=N3)C=C2)C2=C(C(OC(OC(OC3CCCCC3)=O)C)=O)C=CC=C2N=1
Xi'an Eastling biotech Co., Ltd. is dedicated to the research and development, production, and sales of natural plant extracts; With nearly 15 years of experience in identifying, researching, developing, and producing active ingredients for medicinal plants, we focus on providing innovative products and services to customers in industries such as pharmaceuticals, health food, and cosmetics.
Eastling Biotechnology has established a global direct harvesting system for plant raw materials, ensuring the high quality and authenticity of raw materials, while also protecting the continuity and diversity of plants; Having strong research and development capabilities, we can develop more effective and specialized plant active ingredients for the pharmaceutical, health food, and cosmetics industries; We have established an advanced quality control system, and the quality control of our products depends on advanced testing instruments and high-level technical experts. The effective combination of the two forms Eastling's ability to quickly and rigorously control product quality.
We have a production system that complies with Chinese GMP and American cGMP certifications, as well as advanced and optimized large-scale industrial production technology. In addition to producing specific products for Eastling Biotechnology, we also provide customized services to meet the characteristics and needs of different customers to produce customized products.
We believe that natural active ingredients are the foundation of our service to customers. Scientific and effective production technology is the foundation for us to provide customers with specialized products. We have the ability to serve customers in the pharmaceutical, health food, and cosmetics industries, provide new product solutions, and add new value to their products.