(R)-Posenacaftor sodium
(Synonyms: (R)-PTI-801 sodium) 目录号 : GC62513
(R)-Posenacaftor (R)-PTI-801) sodium 是 Posenacaftor 的 R 对映异构体。Posenacaftor (PTI-801) 是一种囊性纤维化跨膜调节蛋白 (CFTR) 调节剂，可纠正 CFTR 蛋白的折叠和运输。Posenacaftor 用于囊性纤维化 (CF) 的研究。
Cas No.:2095064-09-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
(R)-Posenacaftor (R)-PTI-801) sodium is the R enantiomer of Posenacaftor. Posenacaftor is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF)[1].
Cystic fibrosis (CF) is an autosomal recessive disorder, caused by mutations of the cystic fibrosis transmembrane conductance regulator (CFTR)[1].CFTR is a cAMP-regulated chloride channel that is primarily located at the apical membrane of epithelial cells. Mutations in the CFTR gene lead to the production of a defective and misfolded CFTR protein, and impairs the flow of ions in and out of cells[1].Posenacaftor is a CFTR corrector, correctors are designed to fix and restore the function of the defective CFTR protein. The corrected CFTR then moves to the cell surface, where it functions as a chloride channel and helps maintain the right balance of fluid in the airways[2].
[1]. Benjamin Kopp, et al. Compositions et procÉdÉs pour amÉliorer la fonction cftr dans des cellules affectÉes par la fibrose kystique. Patent WO2019156946.
| Cas No. | 2095064-09-6 | SDF | |
| 别名 | (R)-PTI-801 sodium | ||
| 分子式 | C27H26NNaO5 | 分子量 | 467.49 |
| 溶解度 | DMSO : 38.33 mg/mL (81.99 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 | 2.1391 mL | 10.6954 mL | 21.3908 mL |
| 5 mM | 0.4278 mL | 2.1391 mL | 4.2782 mL |
| 10 mM | 0.2139 mL | 1.0695 mL | 2.1391 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。
Renal function and sodium balance in conscious Dahl S and R rats
Am J Physiol 1987 May;252(5 Pt 2):R833-41.PMID:3578550DOI:10.1152/ajpregu.1987.252.5.R833.
Renal transplantation studies have indicated that some form of renal dysfunction underlies the development of hypertension in Dahl salt-sensitive (S) rats. In the present study, we compared renal hemodynamic and tubular function of conscious Dahl S and salt-resistant (R) rats. Prehypertensive Dahl S rats had a blunted natriuretic response to an intravenous isotonic sodium chloride load compared with the responses of normotensive Dahl R or hypertensive Dahl S rats. This difference was probably not related to a generalized defect in renal tubular handling of sodium and water, since prehypertensive Dahl S rats excreted quantities of sodium comparable to those of R or hypertensive S rats when infused with hypertonic sodium chloride solutions. Dahl S rats also elevated free water clearance and lowered urine osmolality similar to R rats when challenged with a hypotonic saline load. Renal blood flows and glomerular filtration rates were similar in prehypertensive Dahl S, hypertensive Dahl S, and Dahl R rats. The possible link between sodium retention and the development of hypertension in Dahl S rats was examined further by measuring the changes in sodium and water balance, extracellular fluid volume (ECV), and blood pressure after exposure to an 8% sodium chloride diet. No differences could be detected in the salt and water balances of Dahl S and R rats exposed to a high-salt diet for 14 days. ECV increased significantly by 10% in Dahl S rats on the 1st day of a high-salt diet, whereas no change was observed in Dahl R animals.(ABSTRACT TRUNCATED AT 250 WORDS)
Sodium microsolvation in ethanol: common features of Na(HO-R)n (R=H, CH3, C2H5) clusters
J Phys Chem A 2011 Jun 16;115(23):6068-76.PMID:21405035DOI:10.1021/jp110584s.
Ethanol clusters are generated in a continuous He seeded supersonic expansion and doped with sodium atoms in a pick-up cell. By this method clusters of the type Na(C(2)H(5)OH)(n) are formed and characterized by determining size selectively their ionization potentials (IPs) for n = 2-40 in photoionization experiments. A continuous decrease to 3.1 eV is found from n = 2 to 6 and a constant value of 3.07 ± 0.06 eV for n = 10-40. This IP evolution is similar to the sodium-water and the sodium-methanol system. Quantum chemical calculations (B3LYP and MP2) of the IPs indicate adiabatic contributions to the photoionization process for the cluster sizes n = 4 and 5, which is similar to the sodium-methanol case. The results of the extrapolated IPs and the vertical binding energies (VEBs) of cluster anions are compared with the recently reported VEBs of solvated electrons in liquid water, methanol, and ethanol solutions in the range of 3.1-3.4 eV. The new results imply that the extrapolated VBEs of solvated electrons in anionic clusters match the VBE in liquid water, while they are about 0.5 eV too low for methanol. The influence of the presence of counterions on these findings is discussed.
Sodium removal during pre-dilution haemofiltration
Nephrol Dial Transplant 2003 Aug;18 Suppl 7:vii31-6; discussion vii57-8.PMID:12953027DOI:10.1093/ndt/gfg1076.
Background: Cardiovascular instability still affects a large percentage of uraemic patients undergoing extracorporeal substitutive treatments. Post-dilution haemofiltration has been reported to be a method for improving cardiovascular stability; however, the limited removal of small molecular weight solutes together with the need for high blood flow from the fistula greatly restrict the use of this treatment. To increase the solute clearances and to partially resolve the necessity for high blood flow, the replacement solution, in a quantity about double that used in post-dilution mode, can be administered in pre-dilution mode. A high vascular stability has also been observed for pre-dilution haemofiltration. Since the lower morbidity may be due to less sodium removal when compared with haemodialysis, it would be important to characterize the sodium transport in this kind of treatment. Methods: Nine patients underwent nine pre-dilution haemofiltration treatments (one for each patient) with on-line prepared substitution fluid. Results: As mean values, total (NaF(pw)) and ionized (NaE(pw)) plasma water sodium concentrations increased from 149.4 +/- 2.8 mEq/l to 151.1 +/- 2.4 mEq/l, and from 143.1 +/- 2.8 to 144.5 +/- 1.2 mEq/l, respectively, during the treatment, suggesting a hypotonic concentration of net ultrafiltrate. Plotting the difference between final and initial ionized plasma water concentrations (fNaE(pw) - iNaE(pw)) against the difference between initial plasma water values and ionized sodium concentration in the reinfusate (iNaE(pw) - NaE(R)), a significant negative correlation was found, with the regression line that intercepts the abscissa at the (iNaE(pw) - NaE(R)) value of 8.8 mEq/l; this means that to avoid changes in NaE(pw) in our patients, the NaE(R) should be lower than the iNaE(pw) by this amount. This is quite different from the theoretical value of approximately 4 mEq/l necessary to avoid changes in NaE(pw) during haemodialysis. The ratio between the total sodium concentration in the ultrafiltrate (NaF(uf)) and NaF(pw) (alpha) at the post-reinfusion site was 0.96 and decreased to 0.94 when NaF(pw) values at the pre-reinfusion site were considered. This last value is quite close to the theoretical alpha value of post-dilution haemofiltration. Conclusion: As for post-dilution haemofiltration, less sodium removal, compared with haemodialysis, can partly explain the improved cardiovascular stability during pre-dilution haemofiltration.
Dialysate sodium and sodium gradient in maintenance hemodialysis: a neglected sodium restriction approach?
Nephrol Dial Transplant 2011 Apr;26(4):1281-7.PMID:21303968DOI:10.1093/ndt/gfq807.
Background: A higher sodium gradient (dialysate sodium minus pre-dialysis plasma sodium) during hemodialysis (HD) has been associated with sodium loading; however, its role is not well studied. We hypothesized that a sodium dialysate prescription resulting in a higher sodium gradient is associated with increases in interdialytic weight gain (IDWG), blood pressure (BP) and thirst. Methods: We conducted a cross-sectional study on 1084 clinically stable patients on HD. A descriptive analysis of the sodium prescription was performed and clinical associations with sodium gradient were analyzed. Results: The dialysate sodium prescription varied widely across dialysis facilities, ranging from 136 to 149 mEq/L, with a median of 140 mEq/L. The mean pre-HD plasma sodium was 136.7 ± 2.9 mEq/L, resulting in the majority of subjects (n = 904, 83%) being dialyzed against a positive sodium gradient, while the mean sodium gradient was 4.6 ± 4.4 mEq/L. After HD, the plasma sodium increased in nearly all patients (91%), reaching a mean post-HD plasma sodium of 141.3 ± 2.5 mEq/L. We found a direct correlation between IDWG and sodium gradient (R = 0.21, P < 0.0001). After adjustment for confounders and clustering by facilities, the sodium gradient was independently associated with IDWG (70 g/mEq/L, P < 0.0001). There were no significant associations among sodium gradient and BP, whether measured as pre-HD systolic (R = -0.02), diastolic (R = -0.06) or mean arterial pressure (R = -0.04). Post-HD thirst was directly correlated with sodium gradient (R = 0.11, P = 0.02). Conclusion: Sodium gradient is associated with statistically significant and clinically meaningful differences in IDWG in stable patients on HD.
Patient self-assessment of urine dipsticks to estimate sodium intake in patients with hypertension
Clin Nutr ESPEN 2022 Oct;51:295-300.PMID:36184219DOI:10.1016/j.clnesp.2022.08.011.
Background & aims: Dietary sodium restriction is recommended by current guidelines to reduce blood pressure and decrease the risk of cardiovascular disease. Current methods to assess sodium intake such as dietary questionnaires and 24-h urine collection are cumbersome, and the results are not readily available to patients. In this analysis, we evaluated using chloride and creatinine dipsticks as a convenient method to monitor sodium intake, in addition to patients' ability to practice this method independently. Methods: This is a post-hoc analysis of a previously published trial, LowSalt4Life, that measured change in sodium consumption over 8 weeks to evaluate the effect of a just-in-time adaptive mobile application intervention. Participants were instructed on how to complete and interpret Quantab® chloride and Multistix® PRO 10 LS creatinine dipstick measurements at home and upload a picture of their results. A pharmacy student interpreted the chloride dipsticks, and intraclass correlation coefficients (ICC) were calculated to assess interrater reliability between the participant and pharmacy student. Predicted 24-h sodium values were calculated by the Kawasaki and Mann methods and compared to actual 24-h sodium excretion. Results: There was a strong interobserver correlation between interpretations of the chloride dipsticks, with the ICC values 0.90, 0.97, 0.99, and 0.98 at weeks 2, 4, 6, and 8, respectively. There was a moderate correlation between the dipstick predicted 24-h sodium excretion and actual 24-h sodium excretion at baseline (R = 0.506; P < 0.001), and a weak correlation at week 8 (R = 0.187; P = 0.217). When corrected creatinine values were used, the dipstick predicted 24-h sodium excretion correlated with the actual 24-h sodium excretion at baseline and week 8 (R = 0.512; P < 0.001 and R = 0.451; P = 0.002). Conclusions: Our analysis suggests that chloride and creatinine dipsticks have the potential to predict total daily excretion of sodium. This method provides patients with an easy, convenient, and accurate method to assess sodium excretion at home. Further research is needed to identify the optimal timing of performing the dipstick analysis as well as ways to improve the creatinine measurement of the urine samples. Trial registration: ClinicalTrials.gov NCT03099343; https://clinicaltrials.gov/ct2/show/NCT03099343.