DOTA-DPhe-Cys-Tyr-DTrp-Lys-Thr-Cys-Thr-ol (trifluoroacetate salt)(Cys2 and 7 bridge)
基本描述
This NYAD-2 peptide is NYAD-1 labeled with FITC (Ex/Em=493/517 nm). NYAD-1 is a cell-penetrating alphalpha-Helical peptide used as a potential HIV-1 inhibitor. The hydrocarbon-stapled structure enhances alpha helicity.
溶解度
分子量
1421.64
化学式
C65H90N14O19S2
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
L.Kolby et al., Br. J. Cancer, 93, 1144 (2005) R.Valkema et al., J. Nucl. Med., 46, 83S (2005) M.de Jong et al., J. Nucl. Med., 46, 13S (2005) W.A.Breeman et al., Eur. J. Nucl. Med. Mol. Imaging, 30, 917 (2003) A.Capello et al., Cancer Biother. Radiopharm., 18, 761 (2003) Chinol, M. et al. Semin. Nucl. Med. 32,141(2002) De Jong, M. et al. semin Nucl. Med. 32,133(2002)
DOTA-DPhe-Cys-Phe-DTrp-Lys-Thr-Cys-Thr-ol (trifluoroacetate salt)(Cys2 and 7 bridge)
基本描述
溶解度
分子量
1405.7
化学式
C65H92N14O17S2
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
L.Kolby et al., Br. J. Cancer, 93, 1144 (2005) R.Valkema et al., J. Nucl. Med., 46, 83S (2005) M.de Jong et al., J. Nucl. Med., 46, 13S (2005) W.A.Breeman et al., Eur. J. Nucl. Med. Mol. Imaging, 30, 917 (2003) A.Capello et al., Cancer Biother. Radiopharm., 18, 761 (2003) Chinol, M. et al. Semin. Nucl. Med. 32,141(2002)
H-DPhe-Cys-Phe-DTrp-Lys-Thr-Cys-Thr-ol (trifluoroacetate salt)(Cys2 and 7 bridge)
基本描述
[Cys2, Tyr3,Orn5,Pen7]. This somatostatin analog is a very potent and highly selective ligand for m-opioid receptors.
溶解度
分子量
1019.2
化学式
C48H66N10O9S2
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
S.Grozinsky-Glasberg et al., Neuroendocrinology, 87, 168 (2008) T.E.Jonassen et al., Am. J. Physiol. Renal Physiol., 291, F537 (2006) H.G.Ding et al., Chin. Med. J., 117, 913 (2004) G.Melacini et al., Biochemistry, 36, 1233 (1997) S.W.Lamberts et al., N. Engl. J. Med., 334, 246 (1996) D. Maouyo et al., Pancreas, 14, 47 (1997) W. Bauer et al., Life Sci, 31(11), 1133 (1982)
Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.
体内研究 (In Vivo)
Octreotide-treated groups show a significant reduction in the tumor volume when compared with saline group. Octreotide-PPSG (1.4 mg/kg, i.p.) shows greater antitumor effect than Octreotide-soln (100 μg/kg, i.p.). Octreotide-treatments results in significant inhibitory effect on the expression levels of SSTR2 and SSTR5 in primary HCC-bearing rats compared with the saline group. Octreotide-PPSG appears to inhibit the expression of SSTR2 and SSTR5 to a greater extent than that of Octreotide-soln treated group[1]. A test dose of octreotide acetate significantly decreases the serum gastrin level to approximately one third of the baseline in 2 hr and the effect lasted approximately for 6 hr. On day 21, treatment with sustained-release formulation of octreotide acetatea (5 mg intramuscular, q 4 wk) is initiated[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
1079.29
Formula
C51H70N10O12S2
CAS 号
79517-01-4
中文名称
醋酸奥曲肽
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisture and light
Powder
-80°C
2 years
-20°C
1 year
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : ≥ 29 mg/mL (26.87 mM)
H2O : 25 mg/mL (23.16 mM; Need ultrasonic)
*“≥” means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
0.9265 mL
4.6327 mL
9.2654 mL
5 mM
0.1853 mL
0.9265 mL
1.8531 mL
10 mM
0.0927 mL
0.4633 mL
0.9265 mL
*
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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
[1]. Wang M, et al. Pharmacokinetic and pharmacodynamic study of a phospholipid-based phase separation gel for once a month administration of octreotide. J Control Release. 2016 May 28;230:45-56.
[2]. Kim S, et al. Treatment of Gastrin-Secreting Tumor With Sustained-Release Octreotide Acetate in a Dog. J Am Anim Hosp Assoc. 2015 Nov-Dec;51(6):407-12.
Animal Administration [1]
Mice[1] Thirty mice with HCC xenografts are randomLy divided into three groups: (A) Octreotide-soln group, (B) Octreotide-PPSG group, and (C) control group. Octreotide-soln group receives i.p. injection of 100 μg/kg octreotide-soln once a day and totally for consecutive 14 days. Octreotide-PPSG group receives a single subcutaneous injection of 1.4 mg/kg Octreotide-PPSG, and the injection volume is about 0.2 mL. Control group receives i.p. injection of saline once a day for consecutive 14 days. Treatment starts on the next day after injection of H22 hepatoma cell suspension and maintains for 14 days. Tumor growth is monitored by periodic caliper measurements on day 7 and day 14 post seeding. Tumor volumes (V) are calculated based on the length and width of tumor by Eq. Rats[1] Twelve male SD rats are divided into two groups, and housed in standard cages at 25°C, with free access to food and water for a week prior to the experiment. Rats are subcutaneously injected with Octreotidereotide solution (Octreotide-soln) or Octreotide-PPSG at an equivalent single dose of 20 mg/kg. The dose is determined based on the clinical dose of Octreotide-soln in human. Rats are fasted for 12 h before dosing and food is returned approximately 2 h post dosing. Blood samples are collected at predetermined time points using heparinized Eppendorf tubes. Immediately after collection, the blood samples are placed on ice until centrifuged at 3000 g for 10 min within 1 h. The plasma is collected and stored at −20°C until analysis.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Wang M, et al. Pharmacokinetic and pharmacodynamic study of a phospholipid-based phase separation gel for once a month administration of octreotide. J Control Release. 2016 May 28;230:45-56.
[2]. Kim S, et al. Treatment of Gastrin-Secreting Tumor With Sustained-Release Octreotide Acetate in a Dog. J Am Anim Hosp Assoc. 2015 Nov-Dec;51(6):407-12.