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Berotralstat HCl

编号: 20619
Cas号: 1809010-52-3
纯度: 98% Min.

Berotralstat HCl is a novel selective inhibitor of plasma kallikrein, blocking the enzymatic activity of plasma kallikrein in releasing bradykinin, the major biologic peptide that promotes swelling and pain associated with attacks of HAE.

仅供研究使用。 我们不向患者出售。

化学信息

名称Berotralstat HCl
Iupac 化学名称1-(3-(aminomethyl)phenyl)-N-(5-((3-cyanophenyl)((cyclopropylmethyl)amino)methyl)-2-fluorophenyl)-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide dihydrochloride
同义词Berotralstat hydrochloride; Berotralstat HCl; Berotralstat dihydrochloride; Berotralstat 2HCl;
英文同义词Berotralstat hydrochloride; Berotralstat HCl; Berotralstat dihydrochloride; Berotralstat 2HCl;
分子式C30H28Cl2F4N6O
分子量635.48
SmileO=C(C1=CC(C(F)(F)F)=NN1C2=CC=CC(CN)=C2)NC3=CC(C(C4=CC=CC(C#N)=C4)NCC5CC5)=CC=C3F.[H]Cl.[H]Cl
InChiKeyXFZLBLTUANGZBD-UHFFFAOYSA-N
InChiInChI=1S/C30H26F4N6O.2ClH/c31-24-10-9-22(28(37-17-18-7-8-18)21-5-1-3-19(11-21)15-35)13-25(24)38-29(41)26-14-27(30(32,33)34)39-40(26)23-6-2-4-20(12-23)16-36;;/h1-6,9-14,18,28,37H,7-8,16-17,36H2,(H,38,41);2*1H
Cas号1809010-52-3
相关CAS号

订购信息

包装价格库存纯度备货期
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外观性状固体粉末
纯度98% Min.
存储短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度
可溶性溶于DMSO
处理方式
运输条件作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周.
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Mathis A, Sale M, Cornpropst M, Sheridan WP, Ma SC. Population pharmacokinetic modeling and simulations of berotralstat for prophylactic treatment of attacks of hereditary angioedema. Clin Transl Sci. 2022 Apr;15(4):1027-1035. doi: 10.1111/cts.13233. Epub 2022 Feb 25. PMID: 35212456; PMCID: PMC9010267.

2: Gao Y, Hwang J, Hwang G, Craig T. A review of oral kallikrein inhibitor berotralstat for hereditary angioedema. Drugs Today (Barc). 2022 Feb;58(2):59-67. doi: 10.1358/dot.2022.58.2.3369191. PMID: 35188140.

3: Anderson J, Maina N. Reviewing clinical considerations and guideline recommendations of C1 inhibitor prophylaxis for hereditary angioedema. Clin Transl Allergy. 2022 Jan 18;12(1):e12092. doi: 10.1002/clt2.12092. PMID: 35079346; PMCID: PMC8764638.

4: Kelbel T. A case of normal C1 esterase inhibitor hereditary angioedema successfully treated with berotralstat. Ann Allergy Asthma Immunol. 2022 Apr;128(4):462-463. doi: 10.1016/j.anai.2022.01.014. Epub 2022 Jan 19. PMID: 35063629.

5: Soteres DF, Grimes F. Patient and caregiver perspectives on transitioning to oral prophylaxis in the emerging hereditary angioedema treatment landscape. Clin Case Rep. 2021 Nov 16;9(11):e05086. doi: 10.1002/ccr3.5086. PMID: 34815876; PMCID: PMC8593787.

6: Orui S, Nozue H, Kobayashi S, Fujioka M, Maekawa Y. [Pharmacological and clinical study results of Berotralstat Hydrochloride for long-term prophylactic treatment of hereditary angioedema]. Nihon Yakurigaku Zasshi. 2021;156(6):382-390. Japanese. doi: 10.1254/fpj.21069. PMID: 34719573.

7: Geng B, Craig TJ. Small molecule drugs for atopic dermatitis, rheumatoid arthritis, and hereditary angioedema. Ann Allergy Asthma Immunol. 2022 Mar;128(3):263-268. doi: 10.1016/j.anai.2021.10.015. Epub 2021 Oct 18. PMID: 34673223.

8: Gower RG, Wilber M. Considerations for transition from subcutaneous to oral prophylaxis in the treatment of hereditary angioedema. Allergy Asthma Clin Immunol. 2021 Oct 9;17(1):100. doi: 10.1186/s13223-021-00603-9. PMID: 34627358; PMCID: PMC8501591.

9: Berotralstat (Orladeyo) for prevention of hereditary angioedema. Med Lett Drugs Ther. 2021 Jul 26;63(1629):e7-e8. PMID: 34544111.

10: Manning ME. Recognition and Management of Hereditary Angioedema: Best Practices for Dermatologists. Dermatol Ther (Heidelb). 2021 Oct;11(5):1829-1838. doi: 10.1007/s13555-021-00593-x. Epub 2021 Aug 30. PMID: 34460082; PMCID: PMC8484417.

11: Kotian PL, Wu M, Vadlakonda S, Chintareddy V, Lu P, Juarez L, Kellogg-Yelder D, Chen X, Muppa S, Chambers-Wilson R, Davis Parker C, Williams J, Polach KJ, Zhang W, Raman K, Babu YS. Berotralstat (BCX7353): Structure-Guided Design of a Potent, Selective, and Oral Plasma Kallikrein Inhibitor to Prevent Attacks of Hereditary Angioedema (HAE). J Med Chem. 2021 Sep 9;64(17):12453-12468. doi: 10.1021/acs.jmedchem.1c00511. Epub 2021 Aug 26. PMID: 34436898.

12: Powell J, Piszczatoski C, Rubido E. Orladeyo (Berotralstat): A Novel Oral Therapy for the Prevention of Hereditary Angioedema. Ann Pharmacother. 2022 Apr;56(4):488-493. doi: 10.1177/10600280211032982. Epub 2021 Jul 20. PMID: 34282650.

13: Farkas H, Stobiecki M, Peter J, Kinaciyan T, Maurer M, Aygören-Pürsün E, Kiani-Alikhan S, Wu A, Reshef A, Bygum A, Fain O, Hagin D, Huissoon A, Jeseňák M, Lindsay K, Panovska VG, Steiner UC, Zubrinich C, Best JM, Cornpropst M, Dix D, Dobo SM, Iocca HA, Desai B, Murray SC, Nagy E, Sheridan WP. Long-term safety and effectiveness of berotralstat for hereditary angioedema: The open-label APeX-S study. Clin Transl Allergy. 2021 Jun;11(4):e12035. doi: 10.1002/clt2.12035. PMID: 34161665; PMCID: PMC8221587.

14: Manning ME, Kashkin JM. Berotralstat (BCX7353) is a novel oral prophylactic treatment for hereditary angioedema: Review of phase II and III studies. Allergy Asthma Proc. 2021 Jul 14;42(4):274-282. doi: 10.2500/aap.2021.42.210034. Epub 2021 Jun 14. PMID: 34127176.

15: Arruda LK, Ferriani MPL. Treatment of hereditary angioedema: When the goal is having a normal life. J Allergy Clin Immunol. 2021 Jul;148(1):80-82. doi: 10.1016/j.jaci.2021.05.023. Epub 2021 May 28. PMID: 34058236.

16: Wedner HJ, Aygören-Pürsün E, Bernstein J, Craig T, Gower R, Jacobs JS, Johnston DT, Lumry WR, Zuraw BL, Best JM, Iocca HA, Murray SC, Desai B, Nagy E, Sheridan WP, Kiani-Alikhan S. Randomized Trial of the Efficacy and Safety of Berotralstat (BCX7353) as an Oral Prophylactic Therapy for Hereditary Angioedema: Results of APeX-2 Through 48 Weeks (Part 2). J Allergy Clin Immunol Pract. 2021 Jun;9(6):2305-2314.e4. doi: 10.1016/j.jaip.2021.03.057. Epub 2021 Apr 15. PMID: 33866032.

17: Lee A. Berotralstat: First Approval. Drugs. 2021 Feb;81(3):405-409. doi: 10.1007/s40265-021-01475-4. PMID: 33646555.

18: Ohsawa I, Honda D, Suzuki Y, Fukuda T, Kohga K, Morita E, Moriwaki S, Ishikawa O, Sasaki Y, Tago M, Chittick G, Cornpropst M, Murray SC, Dobo SM, Nagy E, Van Dyke S, Reese L, Best JM, Iocca H, Collis P, Sheridan WP, Hide M. Oral berotralstat for the prophylaxis of hereditary angioedema attacks in patients in Japan: A phase 3 randomized trial. Allergy. 2021 Jun;76(6):1789-1799. doi: 10.1111/all.14670. Epub 2020 Dec 23. PMID: 33247955; PMCID: PMC8247297.

19: Zuraw B, Lumry WR, Johnston DT, Aygören-Pürsün E, Banerji A, Bernstein JA, Christiansen SC, Jacobs JS, Sitz KV, Gower RG, Gagnon R, Wedner HJ, Kinaciyan T, Hakl R, Hanzlíková J, Anderson JT, McNeil DL, Fritz SB, Yang WH, Tachdjian R, Busse PJ, Craig TJ, Li HH, Farkas H, Best JM, Clemons D, Cornpropst M, Dobo SM, Iocca HA, Kargl D, Nagy E, Murray SC, Collis P, Sheridan WP, Maurer M, Riedl MA. Oral once-daily berotralstat for the prevention of hereditary angioedema attacks: A randomized, double-blind, placebo-controlled phase 3 trial. J Allergy Clin Immunol. 2021 Jul;148(1):164-172.e9. doi: 10.1016/j.jaci.2020.10.015. Epub 2020 Oct 21. PMID: 33098856.

20: Hwang JR, Hwang G, Johri A, Craig T. Oral plasma kallikrein inhibitor BCX7353 for treatment of hereditary angioedema. Immunotherapy. 2019 Dec;11(17):1439-1444. doi: 10.2217/imt-2019-0128. Epub 2019 Oct 22. PMID: 31635497.

化学结构

20619 - Berotralstat HCl | CAS 1809010-52-3

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