연구용
제품 번호S1696
| 관련 타겟 | Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR |
|---|---|
| 기타 Glucocorticoid Receptor 억제제 | Corticosterone AL082D06 (20S)-Protopanaxatriol Cortodoxone |
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| mouse RAW264.7 cells | Function assay | 24 h | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction, IC50=0.061 μM | 21361338 | ||
| mouse L929 cells | Growth inhibition assay | 6 days | Growth inhibition of mouse L929 cells after 6 days | 926113 | ||
| RAW264.7 | Antiinflammatory assay | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production by MTT assay, IC50 = 40.64 μM. | 20879743 | |||
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess reaction based spectrophotometry, IC50 = 40.64 μM. | 21807513 | ||
| RAW264.7 | Function assay | 24 hrs | Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess reaction, IC50 = 40.64 μM. | 23067550 | ||
| RAW264.7 | Antiinflammatory assay | 24 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 43.8 μM. | 23755850 | ||
| L929 | Function assay | 20 hrs | Displacement of 1 x 10'-8 M of [1,2,3-3H]-triamcinolone acetonide from glucocorticoid receptor in soluble fraction of mouse L929 cells after 20 hrs, Kd = 0.043 μM. | 926113 | ||
| HEK293 | Function assay | Inhibition of MR-mediated transactivation of galactosidase reporter gene in HEK293 cells expressing 11betaHSD1 | 16759088 | |||
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of IL-10 production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by ELISA relative to control | 21384845 | |
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of IL-6 production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by ELISA relative to control | 21384845 | |
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of IL1-beta production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by ELISA relative to control | 21384845 | |
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of TNFalpha production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by ELISA relative to control | 21384845 | |
| RAW264.7 | Antiinflammatory assay | 0.5 to 50 ug/ml | 4 hrs | Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production at 0.5 to 50 ug/ml pretreated for 4 hrs followed by challenge with 1 ug/mL LPS for 48 hrs by Griess reaction method relative to control | 21384845 | |
| neural precursor cells | Function assay | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 17417631 | |||
| RAW264.7 | Antiinflammatory assay | 10 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced increase in TNF-alpha level at 10 uM incubated for 2 hrs prior to LPS challenge measured after 22 hrs by ELISA relative to control | 25515561 | |
| RAW264.7 | Antiinflammatory assay | 10 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced increase in IL-6 level at 10 uM incubated for 2 hrs prior to LPS challenge measured after 22 hrs by ELISA relative to control | 25515561 | |
| RAW264.7 | Antiinflammatory assay | 10 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced increase in IL-1beta level at 10 uM incubated for 2 hrs prior to LPS challenge measured after 22 hrs by ELISA relative to control | 25515561 | |
| RAW264.7 | Antiinflammatory assay | 10 uM | 2 hrs | Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production at 10 uM incubated for 2 hrs prior to LPS challenge measured after 22 hrs relative to vehicle-treated control | 25515561 | |
| B16F10 | Apoptosis assay | 20 uM | 36 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increase in cleaved caspase 3 level at 20 uM after 36 hrs by western blot analysis | 26695732 | |
| B16F10 | Apoptosis assay | 20 uM | 36 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increase in p53 expression at 20 uM after 36 hrs by propidium iodide staining based FACS analysis | 26695732 | |
| B16F10 | Apoptosis assay | 20 uM | 36 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increased Bax expression at 20 uM after 36 hrs by western blot analysis | 26695732 | |
| B16F10 | Antitumor activity assay | 6.11 mg/kg | Antitumor activity against mouse B16F10 cells xenografted in C57BL/J mouse assessed as inhibition of tumor growth at 6.11 mg/kg, ip | 26695732 | ||
| B16F10 | Apoptosis assay | 20 uM | 36 hrs | Induction of apoptosis in mouse B16F10 cells assessed as increase in cytochrome C level at 20 uM after 36 hrs by western blot analysis | 26695732 | |
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 362.46 | 화학식 | C21H30O5 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 50-23-7 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | NSC 10483 | Smiles | CC12CCC(=O)C=C1CCC3C2C(CC4(C3CCC4(C(=O)CO)O)C)O | ||
|
In vitro |
DMSO
: 72 mg/mL
(198.64 mM)
Ethanol : 15 mg/mL Water : Insoluble |
|
In vivo |
|||||
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
| Targets/IC50/Ki |
Glucocorticoid receptor
|
|---|---|
| 시험관 내(In vitro) |
Hydrocortisone은 인간 뇌 미세혈관 내피세포주 hCMEC/D3에서 염증 유발 자극(TNF알파 투여)에 대한 내피 장벽 파괴를 방지하며, 이는 부분적으로 오클루딘 수치 유지에 기반한 것으로 입증될 수 있습니다. 이 화합물로 처리된 수지상 세포(DC)는 MHC II 분자, 보조 자극 분자 CD86, DC 특이 마커 CD83의 발현 감소뿐만 아니라 IL-12 분비가 크게 감소합니다. 이는 IFN-감마 생산을 억제하지만 IL-4의 증가된 방출을 유도하고 IL-5에는 변화가 없습니다. 이 화학 물질은 수지상 세포에서 T 세포 증식을 감소시킵니다. 이것은 TNF-알파 유도된 글리코칼릭스의 심각한 분해, 관상동맥 저항 증가, 혈관 누출 및 하이드록시에틸 전분 투과성 증가를 방지하고, 분리된 기니피그 심장에서 비만 세포 탈과립을 유발합니다. 이 화합물은 분리된 기니피그 심장에서 허혈 후 산화 스트레스, 관류 압력 및 삼출물 형성을 감소시킵니다. 이는 허혈 후 신데칸-1, 헤파란 황산염 및 히알루론산의 유출뿐만 아니라 상주 비만 세포로부터의 히스타민 방출을 억제합니다. 이는 IL-4 유도된 생식계 C 엡실론 전사체 수준을 두 배로 증가시키고 성숙한 C 엡실론 mRNA 전사에 필요한 신호를 전달합니다. 이 화학 물질은 IL-4 처리된 B 세포에서 S 뮤-S 엡실론 결손 스위치 재조합을 유도하고, IgM에서 IgG4를 통한 IgE로의 순차적 동형 전환 모델을 지원합니다. |
참조 |
|
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | parkin / AIMP2 CREB |
|
28366931 |
| Immunofluorescence | Glut2 |
|
29717618 |
| Growth inhibition assay | Cell viability |
|
22829975 |
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT05741762 | Active not recruiting | Critical Illness|Adrenal Insufficiency|Septic Shock |
Dr Adnan Agha|United Arab Emirates University |
January 31 2023 | -- |
| NCT05607901 | Recruiting | Dermatologic Disease |
Tanta University |
October 28 2022 | Phase 2 |
| NCT05324618 | Completed | Atopic|Dermatitis |
Ain Shams University|National Hepatology & Tropical Medicine Research Institute |
May 15 2022 | Phase 4 |