Pyridoxylamine dihydrochloride
(Synonyms: 盐酸吡多胺; Pyridoxamine dihydrochloride) 目录号 : GC38366
A 4-methylamine form of vitamin B6
Cas No.:524-36-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Pyridoxylamine is a 4-methylamine form of vitamin B6 that is converted to pyridoxal 5'-phosphate , the active form of vitamin B6, and an important cofactor for metabolism.1 It scavenges isoketals in cell-free assays and inhibits the formation of lysyl-levuglandin-lactam adducts in dazoxiben-stimulated isolated human platelets when used at concentrations of 0.1 and 1 mM.2 Pyridoxylamine (1 g/L in the drinking water) inhibits the development of acellular capillaries and accumulation of Nε-(1-carboxymethyl)-L-lysine in the retina in a rat model of diabetes induced by streptozotocin .3 It reverses STZ-induced deficits in the novel object recognition task in a rat model of diabetes when administered in the drinking water at concentrations of 0.4 and 1 g/L.4
1.Kohlmeier, M.Water-soluble vitamins and nonnutrientsNutrient metabolism567-671(2015) 2.Davies, S.S., Brantley, E.J., Voziyan, P.A., et al.Pyridoxylamine analogues scavenge lipid-derived γ-ketoaldehydes and protect against H2O2-mediated cytotoxicityBiochemistry45(51)(2006) 3.Stitt, A., Gardiner, T.A., Alderson, N.L., et al.The AGE inhibitor Pyridoxylamine inhibits development of retinopathy in experimental diabetesDiabetes51(9)2826-2832(2002) 4.Kassab, S., Begley, P., Church, S.J., et al.Cognitive dysfunction in diabetic rats is prevented by Pyridoxylamine treatment. A multidisciplinary investigationMol. Metab.28107-119(2019)
| Cas No. | 524-36-7 | SDF | |
| 别名 | 盐酸吡多胺; Pyridoxamine dihydrochloride | ||
| Canonical SMILES | OCC1=C(CN)C(O)=C(C)N=C1.[H]Cl.[H]Cl | ||
| 分子式 | C8H14Cl2N2O2 | 分子量 | 241.11 |
| 溶解度 | DMSO : 120 mg/mL (497.70 mM; Need ultrasonic) Water : 120 mg/mL (497.70 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1475 mL | 20.7374 mL | 41.4748 mL |
| 5 mM | 0.8295 mL | 4.1475 mL | 8.295 mL |
| 10 mM | 0.4147 mL | 2.0737 mL | 4.1475 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Pyridoxamine dihydrochloride in diabetic nephropathy (PIONEER-CSG-17): lessons learned from a pilot study
Nephron 2015;129(1):22-8.PMID:25532068DOI:10.1159/000369310.
Background/aims: Pyridoxamine dihydrochloride (Pyridorin™) blocks pathogenic oxidative pathways in the progression of diabetic nephropathy. The pyridoxamine pilot study was designed to test entry criteria and outcomes. Subjects had SCr 1.3-3.5 mg/dl, protein-to-creatinine ≥1,200 mg/g and used a surrogate outcome of ΔSCr over 52 weeks. Subjects had to be on a maximally tolerated dose of ACE/ARB for 3 months; stable other antihypertensive doses for 2 months; stable diuretic dose for 2 weeks, and BP ≤160/90 mm Hg; or enter a Pharmaco-Stabilization Phase (PSP). This pilot failed to detect an effect on ΔSCr in intent-to-treat analysis. Methods: We queried the locked clinical trial database for subgroups in which there was a treatment effect. Results: Subjects not requiring PSP and those with entry SCr <2.0 mg/dl had a treatment effect. Subjects entering PSP required more changes in antihypertensive medications and experienced larger ΔSCr over 52 weeks. PSP subjects with BP >140/90 mm Hg had no treatment effect, but those ≤140/90 mm Hg did. Conclusion: Time required for acute effects of ACE/ARB to stabilize is unknown, but these data suggest >3 months. Thus, subjects in the pivotal trial must be on ACE/ARB for 6 months. Frequent antihypertensive adjustment could engender SCr changes unrelated to CKD progression. Thus, we will require subjects to have BP ≤150/90 mm Hg and on stable antihypertensives for 26 weeks, or ≤140/90 mm Hg and on stable antihypertensives for 13 weeks. Since ΔSCr over 52 weeks is limited as a surrogate outcome, the pivotal trial uses a time-to-event analysis of baseline SCr to at least a 50% increase in SCr or ESRD as the primary outcome. This substantial ΔSCr is protected from noise and is clinically relevant. The pyridoxamine pilot provided critical information to inform the design of PIONEER-CSG-17, which we conducted under the SPA agreement with FDA.
Comparative Study to Evaluate the Effect of Low-Protein Diet Supplementation with Taurine and N-Acetylcysteine, N-Acetylcysteine and Pyridoxamine dihydrochloride in Preventing the Progression of Chronic Renal Failure in Patients with Non-Diabetic Kidney Disease
J Assoc Physicians India 2022 May;70(5):11-12.PMID:35598122doi
Chronic Kidney Disease(CKD) has multifactorial etiology and there are lots of grey zone in understanding its complex pathophysiology. There is no silver bullet for optimal care of CKD. Oxidative stress being well understood and considered as an important common progressive factor for CKD of different etiology. Several research studies focused on reducing oxidative stress and have shown diverse outcomes. In this randomized, open-label, three arms, controlled, single center study we evaluated the role of N acetylcysteine which is a direct scavenger of free radical, in combination with taurine and pyridoxamine in retarding the progression of non-diabetic kidney disease. Methods: 69 non-dialysis, non-diabetic patients diagnosed with chronic renal failure with GFR more than 15 ml/min/1.73m2 and less than 60ml/min/1.73m2 receiving standard of care were enrolled in the study, of which 22 were in the placebo arm, 23 treated with NT (500 mg Taurine + 150 mg NAC) arm and 24 in the NP (300mg NAC+ 50mg pyridoxamine di-hydrochloride) arm. The subjects in the treatment arm received the study drug twice a day along with low protein (0.6gm protein per Kg body weight) isocaloric diet with 25-30 Kcal/Kg/D and were evaluated monthly up to 6 months. Change in eGFR accorss 3 groups over 6 months were compared. Result: Mean age of the subjects was 57 ± 13 years of 56.25% were male and 43.75% were female. 69 patients completed the study. The Empirical Distribution Function (EDF) of NP group was dominant over control and NT group indicating a positive effect of NT on non-diabetic CKD at 10% level of significance. In the subgroup analysis a significant effect was observed in the cases of patients receiving NP with baseline eGFR more than 45 ml/min. The mean increase in eGFR readings over six months was 8.15 units higher in the NP group than in the control group. The two-sided p-values of the t-test, the Wilcoxon test and the Kolmogorov-Smirnov test were 0.0496, 0.0316 and 0.0354, respectively. Thus, all the three tests reject the hypothesis of identical changes in eGFR at the 5% level. In subjects with bicarbonate more than 22 mg/dl, the mean increase in eGFR over six months was 10.86 units higher in the NP group than in the control group indicating NP has a positive effect on increasing eGFR over 6 months, in patients without the presence of any metabolic acidosis. The two-sided p-vales of the t-test, the Wilcoxon test and the Kolmogorov-Smirnov test were 0.0325, 0.0205 and 0.1495, respectively. Thus, two of the three tests reject the hypothesis of identical changes in eGFR at the 5% level which clearly indicates that NP had better efficacy than other groups. Conclusion: N-acetyl cysteine along with pyridoxine may be a useful intervention along with a low protein diet in retarding progression of CKD in the nondiabetic population in early CKD.
Pyridorin in type 2 diabetic nephropathy
J Am Soc Nephrol 2012 Jan;23(1):131-6.PMID:22034637DOI:10.1681/ASN.2011030272.
Pyridoxamine dihydrochloride (Pyridorin, NephroGenex) inhibits formation of advanced glycation end products and scavenges reactive oxygen species and toxic carbonyls, but whether these actions translate into renoprotective effects is unknown. In this double-blind, randomized, placebo-controlled trial, we randomly assigned 317 patients with proteinuric type 2 diabetic nephropathy to twice-daily placebo; Pyridorin, 150 mg twice daily; or Pyridorin, 300 mg twice daily, for 52 weeks. At baseline, the mean age ± SD was 63.9±9.5 years, and the mean duration of diabetes was 17.6±8.5 years; the mean serum creatinine level was 2.2±0.6 mg/dl, and the mean protein-to-creatinine ratio was 2973±1932 mg/g. Regarding the primary end point, a statistically significant change in serum creatinine from baseline to 52 weeks was not evident in either Pyridorin group compared with placebo. However, analysis of covariance suggested that the magnitude of the treatment effect differed by baseline renal function. Among patients in the lowest tertile of baseline serum creatinine concentration, treatment with Pyridorin associated with a lower average change in serum creatinine concentration at 52 weeks (0.28, 0.07, and 0.14 mg/dl for placebo, Pyridorin 150 mg, and Pyridorin 300 mg, respectively; P=0.05 for either Pyridorin dose versus placebo); there was no evidence of a significant treatment effect in the middle or upper tertiles. In conclusion, this trial failed to detect an effect of Pyridorin on the progression of serum creatinine at 1 year, although it suggests that patients with less renal impairment might benefit.
A sensitive UPLC-MS/MS method for simultaneous quantification of one-carbon metabolites & co-factors in human plasma
J Pharm Biomed Anal 2022 Sep 20;219:114944.PMID:35863169DOI:10.1016/j.jpba.2022.114944.
One-carbon metabolism is an important metabolic pathway involved in many diseases, such as congenital malformations, tumours, cardiovascular diseases, anaemia, depression, cognitive diseases and liver disease. However, the current methods have specific defects in detecting and qualifying the related compounds of one-carbon metabolism. In this study, a validated method was established to simultaneously quantify 22 one-carbon metabolites & co-factors in human plasma and applied to the study of correlation between one-carbon metabolism and colorectal cancer in human plasma samples, which were from 44 healthy subjects and 55 colorectal cancer patients. The method used ultra-high performance liquid chromatography coupled with triple quadrupole mass spectrometry (UPLC-MS/MS), and the analytes included betaine, L-carnitine, L-cystathionine, L-cysteine, dimethylglycine, DL-homocysteic acid, homocysteine, methionine, pyridoxal hydrochloride, Pyridoxamine dihydrochloride, pyridoxine dihydrochloride, S-(5'-Adenosyl)-L-homocysteine, serine, choline chloride, folic acid, glycine, pyridoxal phosphate monohydrate, riboflavin, taurine, 5-methyltetrahydrofolate, S-(5'-adenosyl)-L-methionine disulfate salt, trimethylamine oxide. The developed method was successfully applied to the quantification of 22 one-carbon metabolites & co-factors in human plasma from colorectal cancer patients and healthy individuals. The plasma concentrations of dimethylglycine was significantly decreased in the patients compared with the healthy individuals, while L-cystathionine was increased.
Effect of UV Irradiation on the Nutritional Quality and Cytotoxicity of Apple Juice
J Agric Food Chem 2016 Oct 19;64(41):7812-7822.PMID:27632812DOI:10.1021/acs.jafc.6b02491.
UV-C irradiation operating at 254 nm wavelength on the polyphenolic and vitamin contents of apple juice including cytotoxicity analysis was studied. UV doses ranging from 0 to 150 mJ·cm-2 were selected for the treatments. Polyphenols (catechin, epicatechin, chlorogenic acid, and phloridzin) and vitamins (riboflavin, thiamine hydrochloride, pyridoxal hydrochloride, pyridoxine, Pyridoxamine dihydrochloride, cyanocobalamin, choline chloride, biotin, niacin, and niacinamide) were chemically profiled. It was observed that UV treatment of apple juice at disinfection doses caused minor reductions (p < 0.05) in the concentrations of two main polyphenols (i.e., chlorogenic acid and epicatechin). In contrast, significant (p < 0.05) decreases in vitamin concentrations were observed (p < 0.05). The irradiated juice was evaluated for cytotoxic effects. The irradiated apple juice showed no cytotoxic effects on normal intestinal cells, and both irradiated and nonirradiated samples are significantly comparable in inhibiting the growth of human colon cancer cells. Overall, these results indicated that UV-C treatment of apple juice neither significantly degraded polyphenols nor generated cytotoxic compounds.