Seebio 提供从磷脂PEGs到荧光PEGs的多种选择，种类齐全，产品线丰富。同时具备重组蛋白药物中间体合同外包开发和生产（CRO & CDMO）能力。
重组蛋白药物生产流程[1]
利用化学修饰及基因工程技术等对重组蛋白药物进行改造或修饰，解决药物在血液中半衰期短、给药途径单一、免疫原性和毒副反应等问题，进而增强药物活性、提高药效是重组蛋白药物研究的重点之一。长效蛋白质生物制剂技术也是国际上许多大公司抢占的核心技术。
聚乙二醇（PEGs）由于低免疫原性，良好的水溶性及生物相容性，是生物医学中使用最多的聚合物，其“隐身”效应是生物材料的“金标准”。PEGs对蛋白药物修饰途径主要有氨基修饰（包括N端氨基的酰化修饰、赖氨酸侧链氨基的酰化修饰、N端氨基的烷基化修饰）、羧基修饰、巯基修饰等。目前，PEG修饰蛋白质类药物的研究主要集中于腺苷脱氨酶、天冬酰胺酶、干扰素、粒细胞集落刺激因子、白细胞介素等。
CAS# 1188328-37-1
OtBu-Ara-Glu(AEEA-AEEA-OH)-OtBu
(礼来GIP/GLP-1双重激动剂、诺和超级胰岛素)
HO-Ste-CYH-Glu(OH)-Glu(OH)-AEEEEA-Mal
(仅供科研用)
经PEG共价修饰后，蛋白质药物的半衰期得到延长、免疫原性降低，同时最大限度地保留其生物活性，提高了药效：
分子半径增大，肾清除速率下降。
PEG在蛋白表面起到了屏蔽和位阻效应，酶解速率降低，稳定性提高，半衰期延长。
屏蔽和位阻效应还可以掩盖蛋白质表面的抗原位点，降低了蛋白质的免疫原性。
增加了药物在体液中的溶解性。
与药物的化学键在体内随时间水解，缓慢释放药物[2]。
各类PEG化蛋白质[3]
目前重组蛋白药物研发性巨头公司(Amgen、Biogen IDEC、Johnson & Johnson、Eli Lily、Novo Nordisk、Roche)几乎全部来自欧美[4]，占全球市场约80%的比例。而所有欧美公司的销售额占全球生物技术公司销售额高达97%。1990年, FDA批准了, 首个PEG化蛋白质药物，治疗重度免疫缺陷综合征的Adagen (PEG-ADA)以来，许多药物也得到陆续通过审批。
PEGs-modified protein approved FDA. Site-specific PEGylated proteins given in bold [3]
FDA批准的PEG修饰蛋白药物
货号 | CAS | 产品名称 | 纯度 |
AAU0205A | 876345-13-0 | Boc-NH-PEG4-CH2COOH | 97% |
AAU0206A | 951671-87-7 | DNP-PEG3-azide | 98% |
AAU0207A | 112-35-6 | m-PEG3-OH | 97% |
AAU0208A | 756525-95-8 | NH2-PEG2-C2-Boc | 95% |
AAU0209A | 581065-95-4 | Amino-PEG4-Boc | 97% |
AAU0210A | 1393330-38-5 | Bromo-PEG4-acid | 97% |
AAU0211A | 139115-90-5 | Azido-PEG2-alcohol | 97% |
AAU0212A | 86520-52-7 | Azido-PEG3-alcohol | 98% |
AAU0213A | 305372-39-8 | Biotin-PEG2-Mal | 98% |
AAU0214A | 1453117-42-4 | Tos-PEG4-acid | 97% |
AAU0215A | 86259-87-2 | BnO-PEG4-OH | 97% |
AAU0216A | 1312309-63-9 | Azido-PEG2-C2-acid | 97% |
AAU0217A | 1446282-18-3 | Amino-PEG5-Boc | 98% |
AAU0218A | 252881-74-6 | NH2-PEG3-C2-Boc | 97% |
AAU0219A | 1393330-36-3 | Bromo-PEG1-C2-Boc | 97% |
AAU0220A | 928292-69-7 | Amino-PEG10-amine | 97% |
AAU0221A | 890091-43-7 | Boc-amido-PEG9-amine | 97% |
AAU0222A | 1859379-85-3 | Propargyl-PEG2-acid | 98% |
AAU0223A | 906099-89-6 | Biotin-PEG6-alcohol | 97% |
AAU0224A | 1800414-71-4 | Azido-PEG11-amine | 97% |
AAU0225A | 31127-85-2 | Bis-PEG4-acid | 98% |
AAU0226A | 518044-37-6 | Mal-PEG6-Boc | 97% |
AAU0227A | 437655-95-3 | Fmoc-NH-PEG4-CH2COOH | 98% |
AAU0228A | 1122484-77-8 | NH2-PEG2-C1-Boc | 97% |
AAU0229A | 144942-89-2 | Amino-PEG1-C2-acid | 98% |
AAU0230A | 127828-22-2 | Amino-PEG2-NH-Boc | 98% |
AAU0231A | 166388-57-4 | Azido-PEG2-C2-amine | 97% |
AAU0232A | 149299-82-1 | Hydroxy-PEG2-CH2-Boc | 97% |
AAU0233A | 1233234-77-9 | Boc-NH-PEG11-NH2 | 97% |
AAU0234A | 208827-90-1 | Propargyl-PEG3-alcohol | 97% |
AAU0235A | 287174-32-7 | Hydroxy-PEG1-CH2-Boc | 97% |
AAU0236A | 756525-93-6 | Mal-amido-PEG8-NHS ester | 98% |
AAU0237A | 1008402-79-6 | Bis-PEG9-NHS ester | 98% |
AAU0238A | 756526-04-2 | NH2-PEG9-acid | 98% |
AAU0239A | 1191079-83-0 | Amino-PEG9-acid | 97% |
AAU0240A | 872679-70-4 | Fmoc-NH-PEG2-CH2CH2COOH | 98% |
AAU0241A | 882847-13-4 | Boc-NH-PEG6-CH2CH2COOH | 97% |
AAU0242A | 1334169-93-5 | Boc-NH-PEG8-CH2CH2COOH | 97% |
AAU0243A | 756525-91-4 | Boc-NH-PEG4-CH2CH2COOH | 97% |
AAU0244A | 1347750-78-0 | Boc-NH-PEG5-CH2CH2COOH | 97% |
AAU0245A | 1312309-64-0 | N3-PEG2-C2-NHS ester | 97% |
AAU0246A | 439114-13-3 | Bis-PEG5-acid | 97% |
AAU0247A | 875770-34-6 | Biotin-PEG3-azide | 97% |
AAU0248A | 31576-51-9 | m-PEG2-Amine | 98% |
AAU0249A | 1383814-00-3 | Amino-PEG12-Boc | 98% |
AAU0250A | 929-75-9 | Amino-PEG3-C2-Amine | 95% |
AAU0251A | 142929-49-5 | Boc-NH-PEG1-CH2COOH | 97% |
AAU0252A | 937188-59-5 | Hydroxy-PEG4-acid | 97% |
AAU0253A | 663171-32-2 | Biotin-PEG4-amine | 98% |
AAU0254A | 169751-72-8 | Hydroxy-PEG4-CH2-Boc | 97% |
AAU0255A | 2100306-71-4 | Bromo-PEG3-CH2-Boc | 98% |
AAU0256A | 459426-22-3 | Biotin-PEG4-NHS ester | 97% |
AAU0257A | 2055042-66-3 | Hydroxy-PEG9-Boc | 98% |
AAU0258A | 108466-89-3 | Boc-NH-PEG2-CH2COOH | 97% |
AAU0259A | 215181-61-6 | m-PEG2-azide | 97% |
AAU0260A | 86770-67-4 | Azido-PEG4-alcohol | 97% |
AAU0261A | 1895922-74-3 | Boc-NH-PEG2-propargyl | 97% |
AAU0262A | 87450-10-0 | Propargyl-PEG4-alcohol | 95% |
AAU0263A | 9004-74-4 | m-PEG-OH (MW 2000) | 97% |
AAU0264A | 57641-66-4 | Bromo-PEG2-alcohol | 97% |
AAU0265A | 54149-17-6 | m-PEG2-Br | 97% |
AAU0266A | 27425-92-9 | m-PEG10-alcohol | 97% |
AAU0267A | 2101563-45-3 | Fmoc-NH-PEG10-acid | 97% |
AAU0268A | 1257063-35-6 | Azido-PEG4-C2-acid | 97% |
AAU0269A | 462100-06-7 | Boc-NH-PEG3-CH2COOH | 97% |
AAU0270A | 869310-84-9 | Propargyl-PEG2-NHBoc | 97% |
AAU0271A | 858126-78-0 | DNP-PEG4-NHS ester | 97% |
AAU0272A | 518044-31-0 | Hydroxy-PEG3-CH2-Boc | 97% |
AAU0273A | 297162-47-1 | Hydroxy-PEG6-CH2-Boc | 97% |
AAU0274A | 955094-26-5 | Mal-amido-PEG2-NHS ester | 97% |
AAU0275A | 1404111-67-6 | N-Boc-PEG5-alcohol | 97% |
AAU0276A | 186020-66-6 | Hydroxy-PEG3-(CH2)2-Boc | 97% |
AAU0277A | 791028-27-8 | Amino-PEG2-C2-acid | 97% |
AAU0278A | 165963-71-3 | N-Boc-PEG3-bromide | 97% |
AAU0279A | 1334177-79-5 | Mal-amido-PEG6-acid | 97% |
AAU0280A | 2241669-16-7 | NH2-PEG5-C6-Cl (hydrochloride) | 97% |
AAU0281A | 557756-85-1 | Fmoc-NH-PEG4-CH2CH2COOH | 98% |
AAU0282A | 474082-35-4 | Amino-PEG9-amine | 98% |
AAU0283A | 119189-70-7 | Bis-PEG6-acid | 97% |
AAU0284A | 2388521-20-6 | Hydroxy-PEG12-Boc | 98% |
AAU0285A | 361189-64-2 | Hydroxy-PEG6-Boc | 97% |
AAU0286A | 164332-88-1 | N-Boc-PEG2-bromide | 97% |
AAU0287A | 929-59-9 | Bis-NH2-PEG2 | 95% |
AAU0288A | 1818294-42-6 | Amino-PEG10-Boc | 97% |
AAU0289A | 1334177-80-8 | Cbz-NH-PEG6-C2-acid | 97% |
AAU0290A | 957486-82-7 | Azido-PEG6-amine | 97% |
AAU0291A | 1334177-87-5 | Cbz-NH-PEG8-C2-acid | 95% |
AAU0292A | 361189-66-4 | Azido-PEG6-acid | 98% |
AAU0293A | 1670249-37-2 | Azido-PEG9-acid | 98% |
AAU0294A | 39160-70-8 | Amino-PEG6-alcohol | 97% |
AAU0295A | 2093153-98-9 | Propargyl-PEG9-amine | 97% |
AAU0296A | 882518-90-3 | Azido-PEG2-CH2COOH | 97% |
AAU0297A | 756526-00-8 | Cbz-NH-PEG4-C2-acid | 97% |
AAU0298A | 1245823-51-1 | Propargyl-PEG5-acid | 98% |
AAU0299A | 1425973-14-3 | NH2-PEG7 | 98% |
AAU0300A | 1347760-82-0 | Propargyl-PEG3-acid | 97% |
AAU0301A | 1951438-84-8 | Propargyl-PEG6-acid | 97% |
AAU0302A | 932741-19-0 | Propargyl-PEG3-amine | 97% |
AAU0303A | 34188-11-9 | NH2-PEG5-OH | 98% |
AAU0304A | 581065-94-3 | Tos-PEG5-Boc | 97% |
AAU0305A | 86770-68-5 | Azido-PEG5-alcohol | 97% |
AAU0306A | 880129-82-8 | Azido-PEG6-CH2COOH | 98% |
AAU0307A | 1214319-92-2 | Azido-PEG8-acid | 98% |
AAU0308A | 217180-81-9 | Azido-PEG5-CH2CO2H | 98% |
AAU0309A | 857891-82-8 | Azido-PEG8-amine | 97% |
AAU0310A | 5961-83-1 | Bis-PEG1-acid | 98% |
AAU0311A | 19364-66-0 | Bis-PEG2-acid | 97% |
AAU0312A | 2411681-88-2 | Thalidomide-O-PEG4-NHS ester | 97% |
AAU0313A | 82209-36-7 | Amino-PEG8-amine | 98% |
AAU0314A | 1263045-16-4 | Mal-amido-PEG4-acid | 97% |
AAU0315A | 756525-99-2 | Mal-amido-PEG4-NHS ester | 98% |
AAU0316A | 139338-72-0 | Fmoc-amino-PEG3-CH2COOH | 97% |
AAU0317A | 252881-76-8 | Biotin-PEG3-acid | 95% |
AAU0318A | 1381861-91-1 | Bromo-PEG2-C2-Boc | 97% |
AAU0319A | 1292268-13-3 | N-Boc-PEG7-alcohol | 97% |
AAU0320A | 1334286-77-9 | Hydroxy-PEG2-acid | 97% |
AAU0321A | 1036204-60-0 | Propargyl-PEG5-OH | 95% |
AAU0322A | 2250216-93-2 | Boc-NH-PEG3-NHS ester | 97% |
AAU0323A | 1314378-14-7 | Fmoc-PEG4-NHS ester | 98% |
AAU0324A | 1431618-70-0 | Biotin-PEG3-Mal | 97% |
AAU0325A | 912849-73-1 | Azido-PEG10-amine | 97% |
AAU0326A | 157759-50-7 | Bromo-PEG1-CH2-Boc | 97% |
AAU0327A | 134179-38-7 | Amino-PEG3-C2-Azido | 97% |
AAU0328A | 778596-26-2 | Hydroxy-PEG10-Boc | 97% |
AAU0329A | 57641-67-5 | Br-PEG3-OH | 98% |
AAU0330A | 189808-70-6 | NH2-PEG3-C1-Boc | 98% |
AAU0331A | 7218-43-1 | Propargyl-PEG2-OH | 95% |
AAU0332A | 1056024-94-2 | N3-PEG3-CH2CH2COOH | 98% |
AAU0333A | 359860-27-8 | Amine-PEG3-Biotin | 97% |
AAU0334A | 1537892-36-6 | Mal-PEG3-NHS ester | 98% |
AAU0335A | 1260092-44-1 | Boc-NH-PEG1-CH2CH2COOH | 97% |
AAU0336A | 85141-94-2 | Br-PEG4-OH | 97% |
AAU0337A | 352439-37-3 | NH2-PEG8-OH | 97% |
AAU0338A | 141282-35-1 | Amino-PEG5-CH2COOH | 98% |
AAU0339A | 635287-26-2 | Fmoc-NH-PEG5-CH2COOH | 97% |
AAU0340A | 867062-95-1 | Fmoc-NH-PEG3-CH2CH2COOH | 98% |
AAU0341A | 1052207-59-6 | Boc-NH-PEG8-CH2CH2NH2 | 98% |
AAU0342A | 31255-26-2 | Bromo-PEG3-bromide | 98% |
AAU0343A | 24345-74-2 | Azido-PEG1-azide | 98% |
AAU0344A | 1325208-25-0 | Mal-PEG4-NHS ester | 97% |
AAU0345A | 516493-93-9 | Azido-PEG5-amine | 97% |
AAU0346A | 1374666-32-6 | Mal-PEG2-acid | 97% |
AAU0347A | 1013921-36-2 | Propargyl-PEG4-amine | 97% |
AAU0348A | 1347750-75-7 | Boc-N-amido-PEG3-acid | 97% |
AAU0349A | 72236-26-1 | Amino-PEG5-amine | 97% |
AAU0350A | 332941-25-0 | Amino-PEG7-amine | 98% |
AAU0351A | 1517-05-1 | Azido-PEG1 | 97% |
AAU0352A | 945633-30-7 | Biotin-PEG2-CH2CH2N3 | 97% |
AAU0353A | 65869-63-8 | Bis-PEG2-NHS ester | 97% |
AAU0354A | 206265-98-7 | Boc-NH-PEG7-NH2 | 97% |
AAU0355A | 721431-18-1 | Biotin-PEG4-acid | 97% |
AAU0356A | 1027371-75-0 | m-PEG1-NHS ester | 97% |
AAU0357A | 110429-45-3 | m-PEG4-Br | 97% |
AAU0358A | 782475-37-0 | Br-PEG3-C2-Boc | 97% |
AAU0359A | 784105-33-5 | Amino-PEG3-C2-acid | 97% |
AAU0360A | 530151-56-5 | Bromo-PEG2-C2-azide | 97% |
AAU0361A | 905954-28-1 | NH2-PEG6-CH2CH2COOH | 97% |
AAU0362A | 195071-49-9 | Amino-PEG4-CH2COOH | 97% |
AAU0363A | 2365309-92-6 | Cl-PEG6-acid | 98% |
AAU0364A | 1137109-21-7 | Mal-amido-PEG6-NHS ester | 97% |
AAU0365A | 936917-36-1 | Iodo-PEG4-N3 | 97% |
AAU0366A | 85030-56-4 | m-PEG4-Amine | 97% |
AAU0367A | 869718-81-0 | m-PEG8-Amine | 97% |
AAU0368A | 1702356-19-1 | ENdo-BCN-PEG4-NHS ester | 97% |
AAU0369A | 1058691-77-2 | m-PEG6-CH2CH2CHO | 97% |
Seebio Code | CAS No. | Name | |
生长激素侧链 | AAU0178A | N/A | TZ-Ste-SO2-nBu-AEEA-Glu(OH)-Glu(OH)-AEEA-Lys(OH)-C |
AAU0179A | N/A | HO-Ste-CYH-Glu(OH)-Glu(OH)-AEEEEA-Mal | |
Tirzepatide侧链 | AAU0180A | 1188328-37-1 | OtBu-Ara-Glu(AEEA-AEEA-OH)-OtBu |
索马鲁肽侧链 | AAU0181A | 1169630-40-3 | (S)-22-(羧基) -1-((2,5-二氧代环戊基)氧基) -1,10,19,24-四氧代-3,6,12,15-四氧杂-9,18,23-氮杂四十一烷-41-酸 |
AAU0182A | 1118767-16-0 | tBuO-Ste-Glu(AEEA-AEEA-OH)-OtBu | |
AAU0183A | 1118767-15-9 | tBuO-Ste-Glu(AEEA-AEEA-OSu)-OtBu | |
AAU0184A | N/A | tBuO-Ste-Glu(AEEA-AEEA-ONa)-OtBu | |
AAU0185A | 4871-70-5 | 十八烷二酸 | |
AAU0186A | 843666-40-0 | 十八烷二酸单叔丁酯 | |
AAU0187A | 134978-97-5 | AEEA | |
AAU0188A | 1143516-05-5 | AEEA-AEEA | |
AAU0189A | 166108-71-0 | Fmoc-AEEA | |
AAU0190A | N/A | Fmoc-PEG3-乙酸 | |
AAU0191A | 2061897-68-3 | Boc-His(Trt)-Aib-OH | |
AAU0192A | N/A | Boc-His(Trt)-Aib-Glu(OtBu)-Gly-OH | |
AAU0193A | 1662688-20-1 | Fmoc-Lys(tBuO-Ste-Glu(AEEA-AEEA)-OtBu)-OH | |
AAU0194A | N/A | tBuO-Ste-Glu(AEEA-AEEA-Glu)-OtBu | |
利拉鲁肽侧链 | AAU0195A | 204521-63-1 | Pal-Glu(OSu)-OtBu |
AAU0196A | 57078-98-5 | D-Pal-Glu(OSu)-OtBu | |
AAU0197A | N/A | L-HO-Pal-Lys(OSu)-OH | |
AAU0198A | 294855-91-7 | L-Pal-Glu(OSu)-OH | |
AAU0199A | N/A | L-Pal-Glu(OH)-OtBu | |
AAU0200A | N/A | 2L-HO-Pal-Glu(OSu)-OtBu | |
德谷胰岛素侧链 | AAU0201A | N/A | L-HO-Pal-Glu(OSu)-OH |
AAU0202A | N/A | L-tBuO-Pal-Glu(OSu)-OtBu | |
AAU0203A | N/A | L-tBuO-Pal-Glu(OSu)-OH | |
地特胰岛素侧链 | AAU0204A | 69888-86-4 | N-琥珀酰亚胺基豆蔻酸 |
1. Y. Wei, Z.W. Zhang, et al. Chin j Biotech, 2018, 34(3): 360-368
2. K.J. Dozier, D.M. Distefano Int. J. Mol. Sci. 2015, 16(10), 25831-25864(扉页图片)
3. F.M. Veronese, G. Pasut. Drug Discov.Today, 2005, 10(21): 1451–1458
4. W.X. Wu, Y. Zhang, et al. Lett Biotechnol, 2006, 17(6): 929–934.
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